Preparation and characterisation of ciprofloxacin‐loaded silver nanoparticles for drug delivery

Silver nanoparticles (AgNPs) have shown potential applications in drug delivery. In this study, the AgNPs was prepared from silver nitrate in the presence of alginate as a capping agent. The ciprofloxacin (Cipro) was loaded on the surface of AgNPs to produce Cipro‐AgNPs nanocomposite. The characteristics of the Cipro‐AgNPs nanocomposite were studied by X‐ray diffraction (XRD), UV–Vis, transmission electron microscopy (TEM), thermogravimetric analysis (TGA), scanning electron microscopy (SEM), Fourier‐transform infra‐red analysis (FT‐IR) and zeta potential analyses. The XRD of AgNPs and Cipro‐AgNPs nanocomposite data showed that both have a crystalline structure in nature. The FT‐IR data indicate that the AgNPs have been wrapped by the alginate and loaded with the Cipro drug. The TEM image showed that the Cipro‐AgNPs nanocomposites have an average size of 96 nm with a spherical shape. The SEM image for AgNPs and Cipro‐AgNPs nanocomposites confirmed the needle‐lumpy shape. The zeta potential for Cipro‐AgNPs nanocomposites exhibited a positive charge with a value of 6.5 mV. The TGA for Cipro‐AgNPs nanocomposites showed loss of 79.7% in total mass compared to 57.6% for AgNPs which is due to the Cipro loaded in the AgNPs. The release of Cipro from Cipro‐AgNPs nanocomposites showed slow release properties which reached 98% release within 750 min, and followed the Hixson–Crowell kinetic model. In addition, the toxicity of AgNPs and Cipro‐AgNPs nanocomposites was evaluated using normal (3T3) cell line. The present work suggests that Cipro‐AgNPs are suitable for drug delivery.     

Development and in vitro evaluation of oxytetracycline‐loaded PMMA nanoparticles for oral delivery against anaplasmosis

Poly‐methyl methacrylate (PMMA) polymer with remarkable properties and merits are being preferred in various biomedical applications due to its biocompatibility, non‐toxicity and cost effectiveness. In this investigation, oxytetracycline‐loaded PMMA nanoparticles were prepared using nano‐precipitation method for the treatment of anaplasmosis. The prepared nanoparticles were characterised using dynamic light scattering (DLS), atomic force microscopy (AFM), differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy. The mean average diameter of the nanoparticles ranged between 190–240 nm and zeta potential was found to be −19 mV. The drug loading capacity and entrapment efficiency of nanoparticles was found varied between 33.7–62.2% and 40.5–60.0%. The in vitro drug release profile exhibited a biphasic phenomenon indicating controlled drug release. The uptake of coumarin‐6(C‐6)‐loaded PMMA nanoparticles in Plasmodium falciparum (Pf 3D7) culture model was studied. The preferential uptake of C‐6‐loaded nanoparticles by the Plasmodium infected erythrocytes in comparison with the uninfected erythrocytes was observed under fluorescence microscopy. These findings suggest that oxytetracycline‐loaded PMMA nanoparticles were found to be an effective oral delivery vehicle and an alternative pharmaceutical formulation in anaplasmosis treatment, too.Inspec keywords: nanoparticles, nanomedicine, conducting polymers, microorganisms, cellular biophysics, toxicology, drug delivery systems, light scattering, atomic force microscopy, differential scanning calorimetry, Fourier transform infrared spectra, bloodOther keywords: in vitro evaluation, oxytetracycline‐loaded PMMA nanoparticles, anaplasmosis, polymethyl methacrylate polymer, biocompatibility, toxicity, oxytetracycline‐nanoparticles, nanoprecipitation method, dynamic light scattering, atomic force microscopy, AFM, differential scanning calorimetry, DSC, Fourier transform infrared spectroscopy, FTIR spectroscopy, zeta potential, drug loading capacity, entrapment efficiency, in vitro drug release profile, biphasic phenomenon, coumarin‐6(C‐6)‐loaded PMMA nanoparticles, plasmodium falciparum culture model, preferential uptake, plasmodium infected erythrocytes, fluorescence microscopy, oral delivery vehicle, anaplasmosis treatment, size 190 nm to 240 nm     

Polyethylenimine‐modified curcumin‐loaded mesoporus silica nanoparticle (MCM‐41) induces cell death in MCF‐7 cell line

Breast cancer accounts for the first highest mortality rate in India and second in world. Though current treatment strategies are effectively killing cancer cells, they also end in causing severe side effects and drug resistance. Curcumin is a nutraceutical with multipotent activity but its insolubility in water limits its therapeutic potential as an anti‐cancer drug. The hydrophilicity of curcumin could be increased by nanoformulation or changing its functional groups. In this study, curcumin is loaded on mesoporous silica nanoparticle and its anti‐cancer activity is elucidated with MCF‐7 cell death. Structural characteristics of Mobil Composition of Matter ‐ 41(MCM‐41) as determined by high‐resolution transmission electron microscopy (HR‐TEM) shows that MCM‐41 size ranges from 100 to 200 nm diameters with pore size 2–10 nm for drug adsorption. The authors found 80–90% of curcumin is loaded on MCM‐41 and curcumin is released efficiently at pH 3.0. The 50 µM curcumin‐loaded MCM‐41 induced 50% mortality of MCF‐7 cells. Altogether, their results suggested that increased curcumin loading and sustained release from MCM‐41 effectively decreased cell survival of MCF‐7 cells in vitro.Inspec keywords: cancer, cellular biophysics, nanoparticles, nanomedicine, biomedical materials, polymers, mesoporous materials, transmission electron microscopy, drugs, adsorptionOther keywords: polyethylenimine‐modified curcumin‐loaded mesoporus silica nanoparticle, MCF‐7 cell line, breast cancer, cancer cells, drug resistance, multipotent activity, therapeutic potential, anticancer drug, mesoporous silica nanoparticle, MCF‐7 cell death, high‐resolution transmission electron microscopy, drug adsorption, curcumin‐loaded MCM‐41, nutraceutical curcumin, size 2 nm to 10 nm, size 100 nm to 200 nm     

RES‐loaded pegylated CS NPs: for efficient ocular delivery

The objective of this study is to develop resveratrol (RES) loaded polyethylene glycols (PEGs) modified chitosan (CS) nanoparticles (NPs) by ionic gelation method for the treatment of glaucoma. While increasing the concentration of PEG, the particle size and polydispersity index of the formulations increased. Entrapment efficiency and RES loading (RL) of NPs decreased while increasing PEG concentration. The in vitro release of NPs showed an initial burst release of RES (45%) followed by controlled release. Osmolality of formulations revealed that the prepared NPs were iso‐osmolar with the tear. Ocular tolerance of the NPs was evaluated using hen''s egg test on the chorioallantoic membrane and it showed that the NPs were non‐irritant. RES‐loaded PEG‐modified CS NPs shows an improved corneal permeation compared with RES dispersion. Fluorescein isothiocyanate loaded CS NPs accumulated on the surface of the cornea but the PEG‐modified CS NPs crossed the cornea and reached retinal choroid. RES‐loaded PEG‐modified CS NPs reduced the intra‐ocular pressure (IOP) by 4.3 ± 0.5 mmHg up to 8 h in normotensive rabbits. These results indicate that the developed NPs have efficient delivery of RES to the ocular tissues and reduce the IOP for the treatment of glaucoma.Inspec keywords: conducting polymers, nanoparticles, nanomedicine, drug delivery systems, particle size, nanofabrication, organic compounds, biomembranes, cellular biophysics, eye, vision defects, biological tissuesOther keywords: RES‐loaded pegylated CS NP, efficient ocular delivery, resveratrol loaded polyethylene glycol modified chitosan nanoparticles, ionic gelation method, glaucoma treatment, particle size, polydispersity index, entrapment efficiency, RES loading, PEG concentration, in vitro release, osmolality formulations, ocular tolerance, hen egg testing, chorioallantoic membrane, improved corneal permeation, RES dispersion, fluorescein isothiocyanate loaded CS NP, cornea surface, reached retinal choroid, intraocular pressure, normotensive rabbits, RES delivery, ocular tissues     

Evaluation of betamethasone sodium phosphate loaded chitosan nanoparticles for anti‐rheumatoid activity

Nanocarriers, in various forms, have the possibility of providing endless opportunities in the area of drug delivery. The purpose of this study was formulation and evaluation of betamethasone sodium phosphate (BSP) loaded chitosan nanoparticles (CNPs) using cross‐linked chitosan malic acid derivative for better therapeutic effect. The prepared BSP loaded CNPs formulations were characterised for photon correlation spectroscopy, zeta potential, transmission electron microscopy, in‐vitro release kinetics and in‐vivo toxicity studies. Mean particle diameter of BSP loaded CNPs was about 130 nm with spherical morphology. The in‐vitro drug release study of BSP loaded CNPs showed sustained drug release for 48 h and drug release was found to follow zero order. The biochemical, haematology and histopathology reports of in‐vivo toxicity studies revealed that BSP loaded CNPs do not exhibit any toxic effect on vital organs and could be safe. The developed BSP loaded CNPs are found to be safer, and used for the treatments of highly prevalent and chronic disease like rheumatoid arthritis.Inspec keywords: nanoparticles, drug delivery systems, electrokinetic effects, toxicology, photon correlation spectroscopy, transmission electron microscopy, diseases, organic compounds, nanomedicineOther keywords: betamethasone sodium phosphate, chitosan nanoparticles, antirheumatoid activity, nanocarriers, drug delivery, cross‐linked chitosan malic acid derivative, photon correlation spectroscopy, zeta potential, transmission electron microscopy, in‐vitro release kinetics, in‐vivo toxicity, spherical morphology, rheumatoid arthritis     

Formulation and optimisation of lamivudine‐loaded Eudragit® S 100 polymer‐coated pectin microspheres for colon‐specific delivery

This investigation is to find a prolonged or delayed drug release system, exclusively for the treatment of hepatitis‐B to reduce the side effects, which arise when conventional solid dose forms are administered. To pursue this goal, lamivudine‐loaded Eudragit‐coated pectin microspheres have been formulated employing water/oil (W/O) emulsion evaporation strategy. The formulation was optimised using a 3⁴ factorial design. A drug to polymer ratio of 1:2, the surfactant of 1 ml, the volume of 50 ml of processing medium with a stirring speed of 2500 rpm were found to be the optimal parameters to obtain the lamivudine‐loaded Eudragit‐coated pectin microspheres formulation with a high drug entrapment efficiency of 89.44% ± 1.44%. The in vitro release kinetics of lamivudine was a suitable fit to the Higuchi model, indicating a diffusion‐controlled release with anomalous transport. The obtained microspheres were then subjected to different characterisation studies, including scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X‐ray diffraction (XRD). The results of this study clearly indicate that Eudragit‐coated pectin microspheres could be the promising controlled release carriers for colon‐specific delivery of lamivudine in the presence of rat cecal content.     

Controllable synthesis and characterisation of palladium (II) anticancer complex‐loaded colloidal gelatin nanoparticles as a novel sustained‐release delivery system in cancer therapy

Over the past few years, there have been several attempts to deliver anticancer drugs into the body. It has been shown that compared to other available carriers, colloidal gelatin nanoparticles (CGNPs) have distinct properties due to their exceptional physico‐chemical and biological characteristics. In this study, a novel water‐soluble palladium (II) anticancer complex was first synthesised, and then loaded into CGNPs. The CGNPs were synthesised through a two‐step desolvation method with an average particle size of 378 nm. After confirming the stability of the drug in the nanoparticles, the drug‐loaded CGNPs were tested for in vitro cytotoxicity against human breast cancer cells. The results showed that the average drug encapsulating efficiency and drug loading of CGNPs were 64 and 10 ± 2.1% (w/w), respectively. There was a slight shift to higher values of cumulative release, when the samples were tested in lower pH values. In addition, the in vitro cytotoxicity test indicated that the number of growing cells significantly decreased after 48 h in the presence of different concentrations of drug. The results also demonstrated that the released drug could bind to DNA by a static mechanism at low concentrations (0.57 µM) on the basis of hydrophobic and hydrogen binding interactions.Inspec keywords: cancer, drug delivery systems, drugs, palladium compounds, colloids, gelatin, nanoparticles, nanomedicine, biomedical materials, nanofabrication, nanocomposites, molecular biophysics, molecular configurations, pH, solubility, particle size, cellular biophysics, encapsulation, DNA, hydrophobicity, hydrogen bondsOther keywords: controllable synthesis, sustained‐release delivery system, cancer therapy, palladium (II) anticancer complex‐loaded colloidal gelatin nanoparticles, anticancer drug delivery, physicochemical characteristics, biological characteristics, therapeutic pathways, water‐soluble palladium (II) anticancer complex, two‐step desolvation method, particle size, drug stability, gelatin matrix, drug‐loaded CGNPs, in vitro cytotoxic activity, human breast cancer cells, average drug encapsulating efficiency, pH values, cell growth, drug concentrations, DNA, static mechanism, hydrophobic interaction, hydrogen binding interactions     

Investigating preparation and characterisation of diphtheria toxoid‐loaded on sodium alginate nanoparticles

This paper aims to investigate the preparation and characterisation of the alginate nanoparticles (NPs) as antigen delivery system loaded by diphtheria toxoid (DT). For this purpose, both the loading capacity (LC) and Loading efficiency (LE) of the alginate NPs burdened by DT are evaluated. Moreover, the effects of different concentrations of sodium alginate and calcium chloride on the NPs physicochemical characteristics are surveyed in addition to other physical conditions such as homogenization time and rate. To do so, the NPs are characterised using particle size and distribution, zeta potential, scanning electron microscopy, encapsulation efficiency, in vitro release study and FT‐IR spectroscopy. Subsequently, the effects of homogenization time and rate on the NPs are assessed. At the meantime, the NPs LC and efficiency in several DT concentrations are estimated. The average size of the NPs was 400.7 and 276.6 nm for unloaded and DT loaded, respectively. According to the obtained results, the zeta potential of the blank and DT loaded NPs are estimated as −23.7 mV and −21.2 mV, respectively. Whereas, the LC and LE were >80% and >90%, in that order. Furthermore, 95% of the releasing DT loaded NPs occurs at 140 h in the sustained mode without any bursting release. It can be concluded that the features of NPs such as morphology and particle size are strongly depended on the calcium chloride, sodium alginate concentrations and physicochemical conditions in the NPs formation process. In addition, appropriate concentrations of the sodium alginate and calcium ions would lead to obtaining the desirable NPs formation associated with the advantageous LE, LC (over 80%) and sustained in vitro release profile. Ultimately, the proposed NPs can be employed in vaccine formulation for the targeted delivery, controlled and slow antigen release associated with the improved antigen stability.     

Lamivudine‐conjugated and efavirenz‐loaded G2 dendrimers: Novel anti‐retroviral nano drug delivery systems

Infection with human immunodeficiency virus (HIV)‐1 causes immunological disorders and death worldwide which needs to be further assisted by novel anti‐retroviral drug delivery systems. Consequently, finding newer anti‐retroviral pharmaceuticals by using biocompatible, biodegradable nanomaterials comprising a nanoparticle as core and a therapeutic agent is of high global interest. In this experiment, a second generation of a negatively charged nano‐biopolymer linear globular G2 dendrimer was carefully conjugated and loaded with well‐known anti‐HIV drugs lamivudine and efavirenz, respectively. They were characterised by a variety of analytical methods such as Zetasizer, Fourier‐transform infrared spectroscopy, elemental analysis and liquid chromatography‐mass spectroscopy. Additionally, conjugated lamivudine and loaded efazirenz with globular PEGylated G2 dendrimer were tested on an HEK293 T cell infected by single‐cycle replicable HIV‐1 virion and evaluated using XTT test and HIV‐1 P24 protein load. The results showed that lamivudine‐conjugated G2 significantly decreased retroviral activity without any cell toxicity. This effect was more or less observed by efavirenz‐loaded G2. These nano‐constructs are strongly suggested for further in vivo anti‐HIV assays.     

Biosynthesis and characterisation of nano‐silica as potential system for carrying streptomycin at nano‐scale drug delivery

A growing trend within nanomedicine has been the fabrication of self‐delivering supramolecular nanomedicines containing a high and fixed drug content ensuring eco‐friendly conditions. This study reports on green synthesis of silica nanoparticles (Si‐NPs) using Azadirachta indica leaves extract as an effective chelating agent. X‐ray diffraction analysis and Fourier transform‐infra‐red spectroscopic examination were studied. Scanning electron microscopy analysis revealed that the average size of particles formed via plant extract as reducing agent without any surfactant is in the range of 100–170 nm while addition of cetyltrimethyl ammonium bromide were more uniform with 200 nm in size. Streptomycin as model drug was successfully loaded to green synthesised Si‐NPs, sustain release of the drug from this conjugate unit were examined. Prolong release pattern of the adsorbed drug ensure that Si‐NPs have great potential in nano‐drug delivery keeping the environment preferably biocompatible, future cytotoxic studies in this connection is helpful in achieving safe mode for nano‐drug delivery.Inspec keywords: silicon compounds, nanofabrication, nanomedicine, drug delivery systems, nanoparticles, X‐ray diffraction, Fourier transform infrared spectra, scanning electron microscopyOther keywords: nanosilica, streptomycin, nanoscale drug delivery, nanomedicine, silica nanoparticles, Azadirachta indica leaves extract, X‐ray diffraction analysis, Fourier transform‐infrared spectroscopy, scanning electron microscopy, cetyltrimethyl ammonium bromide, SiO₂      

Synthesis and characterisation of PEG modified chitosan nanocapsules loaded with thymoquinone

Thymoquinone (TQ), a major bioactive compound of Nigella sativa seeds has several therapeutic properties. The main drawback in bringing TQ to therapeutic application is that it has poor stability and bioavailability. Hence a suitable carrier is essential for TQ delivery. Recent studies indicate biodegradable polymers are potentially good carriers of bioactive compounds. In this study, polyethylene glycol (PEG) modified chitosan (Cs) nanocapsules were developed as a carrier for TQ. Aqueous soluble low molecular weight Cs and PEG was selected among different biodegradable polymers based on their biocompatibility and efficacy as a carrier. Optimisation of synthesis of nanocapsules was done based on particle size, PDI, encapsulation efficiency and process yield. A positive zeta potential value of +48 mV, indicating good stability was observed. Scanning electron microscope and atomic‐force microscopy analysis revealed spherical shaped and smooth surfaced nanocapsules with size between 100 to 300 nm. The molecular dispersion of the TQ in Cs PEG nanocapsules was studied using X‐ray powder diffraction. The Fourier transform infrared spectrum of optimised nanocapsule exhibited functional groups of both polymer and drug, confirming the presence of Cs, PEG and TQ. In vitro drug release studies showed that PEG modified Cs nanocapsules loaded with TQ had a slow and sustained release.Inspec keywords: nanomedicine, drug delivery systems, polymers, scanning electron microscopy, electrokinetic effects, atomic force microscopy, X‐ray diffraction, Fourier transform infrared spectraOther keywords: PEG modified chitosan nanocapsules, thymoquinone, bioactive compound, Nigella sativa seeds, bioavailability, polyethylene glycol, molecular weight, zeta potential, scanning electron microscope, atomic force microscopy, molecular dispersion, X‐ray powder diffraction, Fourier transform infrared spectrum     

Development of tamoxifen‐loaded surface‐modified nanostructured lipid carrier using experimental design: in vitro and ex vivo characterisation

The present study aimed to develop a surface‐modified biocompatible nanostructured lipid carrier (NLCs) system using polyoxyethylene (40) stearate (POE‐40‐S) to improve the oral bioavailability of poorly water‐soluble Biopharmaceutics Classification System class‐II drug like tamoxifen (TMX). Also aimed to screen the most influential factors affecting the particle size (PS) using Taguchi (L₁₂ (2¹¹)) orthogonal array design (TgL₁₂ OA). Then, to optimize the TMX loaded POE‐40‐S (P) surface‐modified NLCs (TMX‐loaded‐PEG‐40‐S coated NLC (PNLCs) or PNLCs) by central composite design (CCD) using a four‐factor, five‐level model. The most influential factors affecting the PS was screened and optimized. The in‐vitro study showed that increased drug‐loading (DL) and encapsulation efficiency (EE), decreased PS and charge, sustained drug release for the prolonged period of the time with good stability and suppressed protein adsorption. The Ex‐vivo study showed that decreased mucous binding with five‐fold enhanced permeability of PNLC formulation after surface modification with POE‐40‐S. The in‐vitro cytotoxicity study showed that the blank carrier is biocompatible and cytotoxicity of the formulation was dependent on the concentration of the drug. Finally, it can be concluded that the surface‐modified PNLCs formulation was an effective, biocompatible, stable formulation in the enhancement of dissolution rate, solubility, stability with reduced mucus adhesion and increased permeability thereby which indicates its enhanced oral bioavailability.Inspec keywords: nanoparticles, cellular biophysics, solubility, drug delivery systems, toxicology, adsorption, adhesion, dissolving, biomedical materials, encapsulation, polymers, proteins, nanomedicine, permeability, particle size, electrokinetic effectsOther keywords: water‐soluble BCS class‐II, TgL₁₂ OA, TMX‐loaded POE‐40‐S surface‐modified NLC, surface‐modified PNLC formulation, lipid‐based NLC system, oral bioavailability, stable formulation, biocompatible formulation, blank carrier, in vitro cytotoxicity, surface modification, PNLC formulation, drug release, central composite design, orthogonal array design, encapsulation efficiency, steric stabilisation effect, particle size, dissolution rate, polyoxyethylene stearate, surface‐modified biocompatible carrier system, systemic toxicity, water‐soluble drug, tamoxifen‐loaded surface‐modified nanostructured lipid carrier     

Synthesis,characterisation and anti‐tumour activity of biopolymer based platinum nanoparticles and 5‐fluorouracil loaded platinum nanoparticles

A facile and green synthesis of platinum nanoparticles [gum kondagogu platinum nanoparticles (GKPtNP)] using biopolymer‐ gum kondagogu was developed. The formation of GKPtNP was confirmed by ultraviolet (UV)–visible spectroscopy, scanning electron microscopy–energy dispersive X‐ray spectroscopy, transmission electron microscopy, X‐ray diffraction, Zeta potential, Fourier transform infrared, inductively coupled plasma mass spectroscopy. The formed GKPtNP are well dispersed, homogeneous with a size of 2–4 ± 0.50 nm, having a negative zeta potential (−46.1 mV) indicating good stability. 5‐Fluorouracil (5FU) was loaded onto the synthesised GKPtNP, which leads to the development of a new combination of nanomedicine (5FU–GKPtNP). The in vitro drug release studies of 5FU–GKPtNP in pH 7.4 showed a sustained release profile over a period of 120 min. Agrobacterium tumefaciens induced in vitro potato tumour bioassay was employed for screening the anti‐tumour potentials of GKPtNP, 5FU, and 5FU–GKPtNP. The experimental results suggested a complete tumour inhibition by 5FU–GKPtNP at a lower concentration than the GKPtNP and 5FU. Furthermore, the mechanism of anti‐tumour activity was assessed by their interactions with DNA using agarose gel electrophoresis and UV‐spectroscopic analysis. The electrophoresis results revealed that the 5FU–GKPtNP totally diminishes DNA and the UV‐spectroscopic analysis showed a hyperchromic effect with red shift indicating intercalation type of binding with DNA. Over all, the present study revealed that the combined exposure of the nanoformulation resulted in the enhanced anti‐tumour effect. Inspec keywords: nanoparticles, transmission electron microscopy, biomedical materials, tumours, ultraviolet spectra, DNA, drugs, electrophoresis, polymers, platinum, pH, drug delivery systems, biochemistry, X‐ray chemical analysis, microorganisms, molecular biophysics, electrokinetic effects, X‐ray diffraction, scanning electron microscopy, cancer, nanofabrication, visible spectra, nanomedicine, Fourier transform infrared spectra, materials preparationOther keywords: 5FU–GKPtNP, 5‐fluorouracil loaded platinum nanoparticles, gum kondagogu platinum nanoparticles, antitumour activity, scanning electron microscopy‐energy dispersive X‐ray spectroscopy, biopolymer‐based platinum nanoparticles, biopolymer‐based platinum nanoparticles, ultraviolet‐visible spectroscopy, UV‐visible spectroscopy, transmission electron microscopy, X‐ray diffraction, zeta potential, Fourier transform infrared spectroscopy, inductively coupled plasma mass spectroscopy, nanomedicine, in vitro drug release studies, sustained release profile, Agrobacterium tumefaciens, in vitro potato tumour bioassay, tumour inhibition, tumour activity, agarose gel electrophoresis, UV‐spectroscopic analysis, DNA, time 120.0 min, Pt     

Docetaxel‐loaded solid lipid nanoparticles: a novel drug delivery system

Over the past few years, taxanes have emerged as a new class of anticancer drugs. Docetaxel (DTX) the prototype of this class has been approved for the treatment of broad range of cancers. However, to date the commercial preparation of DTX (Taxotere^®) is accompanying adverse side effects, intolerance, and poor solubility, which can be overcome by encapsulating them using solid lipid nanoparticles (SLNs). SLNs represent versatile delivery system of drugs with newer forms such as polymer–solid lipid hybrid, surface modified and long circulating nanoparticles bringing forth improved prospects for cancer chemotherapy. In this review, the authors have discussed the current uses of various SLNs formulations of DTX with key emphasis on controlled and site‐specific drug delivery along with enhanced antitumour activity elucidated via in vitro and in vivo studies. Furthermore, the review article highlights few approaches that can be used in combination with existing DTX‐loaded SLNs to supplement DTX drug delivery.Inspec keywords: nanoparticles, nanomedicine, drug delivery systems, biomedical materials, cancer, reviews, tumoursOther keywords: docetaxel‐loaded solid lipid nanoparticles, drug delivery system, taxanes, anticancer drugs, Taxotere, SLN encapsulation, polymer‐solid lipid hybrid, surface modified nanoparticles, long circulating nanoparticles, chemotherapy, review     

Synthesis of biotin‐targeted chitosan/poly (methyl vinyl ether‐alt ‐maleic acid) copolymeric micelles for delivery of doxorubicin

Biotinylated chitosan/poly(methyl vinyl ether‐alt ‐maleic acid) (PMVEMA) copolymer was synthesised by an amide reaction in two steps. Structural characterisation was performed using ¹ HNMR and Fourier transform infra‐red (FTIR) spectra. Critical micelle concentration (CMC) of the copolymer was determined by pyrene as a fluorescent probe. Doxorubicin (DOX) was loaded in the micelles by the direct dissolution method. The effects of different variables including type of copolymer, copolymer concentration, stirring rate and stirring time were studied on the physicochemical properties of the micelles including: particle size, zeta potential, release efficiency and loading efficiency of nanoparticles using an irregular factorial design. The in vitro cytotoxicity of DOX‐loaded biotin‐targeted micelles was studied in HepG2 cells which over express biotin receptors by 3, 5‐[dimethylthiazol‐2‐yl]‐2, 5‐diphenyl tetrazolium bromide assay. The successful synthesis of the biotinylated copolymer of chitosan/PMVEMA was confirmed by FTIR and ¹ HNMR. The optimised micelles showed the CMC of 33 μg/ml, particle size of 247 ± 2 nm, zeta potential of +9.46 mV, polydispersity index of 0.22, drug‐loading efficiency of 71% and release efficiency of 84.5 ± 1.6%. The synthesised copolymer was not cytotoxic. The cytotoxicity of DOX‐loaded in targeted micelles on HepG2 cell line was about 2.2‐fold compared with free drug.Inspec keywords: biomedical materials, cellular biophysics, dissolving, drug delivery systems, drugs, electrokinetic effects, fluorescence, Fourier transform infrared spectra, particle size, polymer blends, spectrochemical analysis, toxicologyOther keywords: ¹ HNMR spectra, biotin‐targeted chitosan‐poly (methyl vinyl ether‐alt‐maleic acid) copolymeric micelles, doxorubicin delivery, amide reaction, structural characterisation, Fourier transform infrared spectra, pyrene, fluorescent probe, direct dissolution method, physicochemical properties, particle size, zeta potential, nanoparticles, irregular factorial design, in vitro cytotoxicity, DOX‐loaded biotin‐targeted micelles, 3, 5‐[dimethylthiazol‐2‐yl]‐2, 5‐diphenyl tetrazolium bromide assay, polydispersity index, drug‐loading efficiency, HepG2 cell line, voltage 9.46 mV     

Preparation and characterisation of silica‐based nanoparticles for cisplatin release on cancer brain cells

In the present work, the preparation, characterisation, and efficiency of two different silica nanostructures as release vehicles of Cisplatin are reported. The 1‐hexadeciltrimethyl‐ammonium bromide templating agent was used to obtain mesoporous silica nanoparticles which were later loaded with Cisplatin. While sol–gel silica was very fast prepared using an excess of acetic acid during the hydrolysis–condensation reactions of tetraethylorthosilicate and at the same time the Cisplatin was added. Several physicochemical techniques including spectroscopies, electronic microscopy, X‐ray diffraction, N₂ adsorption–desorption were used to characterise the silica nanostructures. An in vitro Cisplatin release test was carried out using artificial cerebrospinal fluid. Finally, the toxicity of all silica nanostructures was tested using the C6 cancer cell line. The spectroscopic results showed the suitable stabilisation of Cisplatin into the two different silica nanostructures. A large surface area was obtained for the mesoporous silica nanoparticles, while low areas were obtained in the silica nanoparticles. Cisplatin was released faster from mesoporous silica channels than from inside of aggregates nanoparticles silica. Cisplatin alone, as well as, cisplatin released from both silica nanostructures exerted a toxic effect on cancer cells. In contrast, both silica structures without the drug did not exert any toxic effect.Inspec keywords: cellular biophysics, desorption, adsorption, biomedical materials, sol‐gel processing, silicon compounds, cancer, toxicology, nanofabrication, brain, condensation, mesoporous materials, nanoparticles, X‐ray diffraction, nanomedicine, drugs, aggregates (materials)Other keywords: mesoporous silica channels, silica‐based nanoparticles, cancer brain cells, silica nanostructures, 1‐hexadeciltrimethyl‐ammonium bromide, mesoporous silica nanoparticles, sol‐gel silica, C6 cancer cell line, in vitro cisplatin release test, C6 cancer cell line, acetic acid, hydrolysis‐condensation reactions, tetraethylorthosilicate, physicochemical techniques, electronic microscopy, X‐ray diffraction, N₂ adsorption‐desorption, artificial cerebrospinal fluid, toxicity, toxic effect, N₂ , SiO₂      

Acyl modified chitosan derivatives for oral delivery of insulin and curcumin

In the present investigation, bioadhesive property of chitosan (CS) was enhanced by the N-acylation with hexanoyl, lauroyl and oleoyl chlorides. The chemical structure of the modified polymer was characterized by FTIR and zeta potential measurements. The swelling ability was evaluated at alkaline pH. Mucin interactions and mucoadhesion experiments were performed under in vitro experimental conditions. Cytotoxicity experiments were employed to confirm the applicability of these particles as drug carriers. Finally in vitro evaluation of hydrophobic and hydrophilic drug release profile at acidic and alkaline pH was also conducted. A strong interaction between CS acyl derivatives and mucin was detected, which was further confirmed by an in situ mucoadhesion experiments with excised intestinal tissue. CS modified with oleoyl chloride showed better mucoadhesion property, as compared to the one modified with lower fatty acid groups. CS derivatives were found non-toxic on L-929 cell lines and provided sustained release of hydrophobic drugs under in vitro experimental conditions. From these studies it seems that hydrophobically modified CS is an interesting system for drug delivery applications.     

用于肺部给药的壳聚糖空心微球的制备

采用壳聚糖为壁材、烷基多糖苷为赋形剂通过喷雾干燥的方法成功制备出了可用于肺部给药的空心载药微球,其粒径在10μm左右。采用扫描电子纤维镜观察了所得粒子的形貌,并分析了喷雾干燥条件下得到这种薄壁空心结构的原理。     

Fabrication of microcapsules with core‐shell structure for oral delivery of dual drugs and real‐time computed tomography imaging

Although multidrug combinations are an effective therapeutic strategy for serious disease in clinical practice, their therapeutic effect may be reduced because they conflict with each other medicinally in certain cases. Hence, there is an urgent need to develop a single drug carrier for precise multidrug delivery to avoid this interference. A reverse coordination method is reported that fabricates a double‐layer barium sulphate microcapsule (DL@BS MS) for two drugs separately loading simultaneously. In addition, BS nanoclusters were synthesised in situ inside the DL@BS MSs for real‐time computed tomography (CT) imaging. The results showed that the DL@BS MSs with a particle size of approximately 2 mm exhibited a uniform sphere. Because BS nanoclusters have a high X‐ray attenuation coefficient, the retention of DL@BS MSs in the digestive tract could be monitored through CT imaging in real time. More important, the core‐shell structure of DL@BS MSs encapsulating two different drugs could be released in spatiotemporal order in an acidic stomach environment. The as‐synthesis DL@BS MSs with a core‐shell structure and real‐time imaging performance provide an ideal carrier for the oral administration of multiple drugs simultaneously loaded but sequentially released.     

壳聚糖-固态分散体载药微球的制备及性能研究

首先采用不同分子量的壳聚糖通过乳化-化学交联法制备了4种不同的壳聚糖载药微球。通过对微球的粒径、溶胀率、载药率、包封率等指标检测以及缓释性能的研究,发现分子量为240kDa的壳聚糖制备的载药微球缓释效果明显,载药率、包封率均较高,综合性能优于其它分子量壳聚糖制备的微球。利用该分子量壳聚糖包埋固态分散体制备了壳聚糖-固态分散体载药微球,改善了药物的溶解性并具有药物缓释作用。因此,壳聚糖-固态分散体载药微球是一种理想的药物缓释体系,可以用于包埋溶解性差,生物半衰期短,对胃肠刺激性强的药物。