Temperature/pH/magnetic triple‐sensitive nanogel–hydrogel nanocomposite for release of anticancer drug

Hydrogels, nanogels and nanocomposites show increasing potential for application in drug delivery systems due to their good chemical and physical properties. Therefore, we were encouraged to combine them to produce a new compound with unique properties for a long‐term drug release system. In this regard, the design and application of a nanocomposite hydrogel containing entrapped nanogel for drug delivery are demonstrated. To this aim, we first prepared an iron oxide nanocomposite nanogel based on poly(N‐isopropylacrylamide)‐co‐((2‐dimethylaminoethyl) methacrylate) (PNIPAM‐co‐PDMA) grafted onto sodium alginate (NaAlg) as a biocompatible polymer and iron oxide nanoparticles (ION) as nanometric base (PND/ION‐NG). This was then added into a solution of PDMA grafted onto NaAlg. Through dropwise addition of mixed aqueous solution of iron salts into the prepared polymeric solution, a novel hydrogel nanocomposite with excellent pH, thermal and magnetic responsivity was fabricated. The synthesized samples were fully characterized using Fourier transform infrared spectroscopy, thermogravimetric analysis, scanning electron microscopy with energy‐dispersive X‐ray analysis, vibrating sample magnetometry and atomic force microscopy. A mechanism for the formation of PNIPAM‐co‐PDMA/NaAlg‐ION nanogel–PDMA/NaAlg‐ION hydrogel and PND/ION nanogel is suggested. Swelling capacity was measured at various temperatures (25 to 45 °C), pH values (from 2 to 11) and magnetic field and under load (0.3 psi) and the dependence of swelling properties of the nanogel–hydrogel nanocomposite on these factors was well demonstrated. The release rate of doxorubicin hydrochloride (DOX) as an anticancer drug was studied at different pH values and temperatures in the presence and absence of a magnetic field. The results showed that these factors have a high impact on drug release from this nanocomposite. The result showed that DOX release could be sustained for up to 12.5 days from these nanocomposite hydrogels, significantly longer than that achievable using the constituent hydrogel or nanogel alone (<1 day). The results indicated that the nanogel–hydrogel nanocomposite can serve as a novel nanocarrier for anticancer drug delivery. © 2019 Society of Chemical Industry     

Controlled co‐delivery of hydrophilic and hydrophobic drugs from thermosensitive and crystallizable copolymer nanoparticles

Functionalized amphiphilic block copolymers poly(N‐isopropyl acrylamide)‐b‐poly(stearyl methacrylate) (PNIPAM‐PSMA) are synthesized. Their self‐assembled core‐shell nanoparticles have the hydrophilic thermosensitive shell and hydrophobic crystallizable core. Nanoparticles exhibit volume phase transition at temperature of 38 °C and its poly(stearyl methacrylate) (PSMA) moiety could form nano size crystals to retain drugs, making them good carriers for drug co‐delivery system. Thermosensitivity and crystallinity of nanoparticles are characterized with dynamic light scattering (DLS), differential scanning calorimetry (DSC), small‐angle X‐ray scattering (SAXS), and atomic force microscopy (AFM). The interactions and relationship between chemical structures of copolymer nanoparticles and loading drugs are discussed. Different loading techniques and combined loading of hydrophobic/hydrophilic drugs are studied. Nanoparticles show a good and controllable drug loading capacity (DL) of hydrophilic/hydrophobic drugs. The drugs release kinetics is analyzed with Fick's law and Weibull model. A general method for analyzing drug release kinetics from nanoparticles is proposed. Weibull model is well fitted and the parameters with definite physical meaning are analyzed. PNIPAM‐PSMA nanoparticles show a quite different thermal response, temporal regulation, and sustained release effect of hydrophilic and hydrophobic drugs, suggesting a promising application in extended and controlled co‐delivery system of multi‐drug. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 44132.     

Lamotrigine‐loaded polyacrylate nanoparticles synthesized through emulsion polymerization

A series of copolymeric nanoparticles of the partially water‐soluble monomer ethyl methacrylate and the water‐soluble monomer 2‐hydroxyl ethyl methacrylate were synthesized from emulsions containing sodium dodecyl sulfate via free‐radical polymerization. Lamotrigine, as a model drug, was loaded in nanoparticles during in situ polymerization. A stable and transparent poly(ethyl methacrylate‐co‐hydroxyl ethyl methacrylate) nanolatex was produced for all compositions and characterized for particle size by dynamic light scattering and transmission electron microscopy. Particles were found to be smaller than 50 nm in size. Structural characterization of copolymers was done by infrared spectrometry, gel permeation chromatography, and NMR spectroscopy. Drug encapsulation efficiency was determined by ultraviolet (UV)–visible spectrometry and was found to be 26–62% for copolymers with different compositions. UV data suggest molecular‐level dispersion of the drug in the nanoparticles. In vitro drug‐release studies showed the controlled release of lamotrigine. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci, 2008     

Preparation of new dendrimer‐like star‐shaped amphiphilic poly(ethylene glycol)–poly(ϵ‐caprolactone) copolymers for biocompatible and high‐efficiency curcumin delivery

Novel amphiphilic star‐shaped terpolymers comprised of hydrophobic poly(?‐caprolactone), pH‐sensitive polyaminoester block and hydrophilic poly(ethylene glycol) (M_n = 1100, 2000 g mol^?1) were synthesized using symmetric pentaerythritol as the core initiator for ring‐opening polymerization (ROP) reaction of ?‐caprolactone functionalized with amino ester dendrimer structure at all chain ends. Subsequently, a second ROP reaction was performed by means of four‐arm star‐shaped poly(?‐caprolactone) macromer with eight ‐OH end groups as the macro‐initiator followed by the attachment of a poly(ethylene glycol) block at the end of each chain via a macromolecular coupling reaction. The molecular structures were verified using Fourier transform infrared and ¹H NMR spectroscopies and gel permeation chromatography. The terpolymers easily formed core–shell structural nanoparticles as micelles in aqueous solution which enhanced drug solubility. The hydrodynamic diameter of these agglomerates was found to be 91–104 nm, as measured using dynamic light scattering. The hydrophobic anticancer drug curcumin was loaded effectively into the polymeric micelles. The drug‐loaded nanoparticles were characterized for drug loading content, encapsulation efficiency, drug–polymer interaction and in vitro drug release profiles. Drug release studies showed an initial burst followed by a sustained release of the entrapped drug over a period of 7days at pH = 7.4 and 5.5. The release behaviours from the obtained drug‐loaded nanoparticles indicated that the rate of drug release could be effectively controlled by pH value. Altogether, these results demonstrate that the designed nanoparticles have great potential as hydrophobic drug delivery carriers for cancer therapy. © 2015 Society of Chemical Industry     

A novel approach to prepare etoposide‐loaded poly(N‐vinyl caprolactam‐co‐methylmethacrylate) copolymeric nanoparticles and their controlled release studies

A series of copolymeric nanoparticles of methyl methacrylate and N‐vinylcaprolactam were synthesized from microemulsions containing sodium dodecyl sulfate. Etoposide as a model drug was loaded in nanoparticles during in situ polymerization. Stable nanolatex were produced and characterized for size and shape by dynamic light scattering (DLS) and transmission electron microscopy. Particles were found to be spherical in nature with size less than 50 nm. Structural characterization of copolymers was done by infrared and nuclear magnetic resonance spectroscopy. Differential scanning calorimetery (DSC) and X‐ray diffractometry (XRD) techniques were used to evaluate molecular level interaction of etoposide with nanoparticles. Drug encapsulation efficiency was determined by ultraviolet (UV) spectrometry and found to be 35–67%. DSC, XRD, and UV data suggested the molecular level dispersion of drug in the nanoparticles. In vitro release studies and in vitro cytotoxicity showed prolonged and controlled release of etoposide from nanoparticles along with IC₅₀ values of nanoparticles in the range of 0.01–0.1 mg/mL. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2013     

PEGylated hollow pH‐responsive polymeric nanocapsules for controlled drug delivery

Novel pH‐responsive PEGylated hollow nanocapsules (HNCaps) were fabricated through a combination of distillation–precipitation copolymerization and surface thiol–ene ‘click’ grafting reaction. For this purpose, SiO₂ nanoparticles were synthesized using the Stöber approach, and then modified using 3‐(trimethoxysilyl)propyl methacrylate (MPS). Afterward, a mixture of triethyleneglycol dimethacrylate (as crosslinker), acrylic acid (AA; as pH‐responsive monomer) and MPS‐modified SiO₂ nanoparticles (as sacrificial template) was copolymerized using the distillation–precipitation approach to afford SiO₂@PAA core–shell nanoparticles. The SiO₂ core was etched from SiO₂@PAA using HF solution, and the obtained PAA HNCaps were grafted with a thiol‐end‐capped poly(ethylene glycol) (PEG) through a thiol–ene ‘click’ reaction to produce PAA‐g‐PEG HNCaps. The fabricated HNCaps were loaded with doxorubicin hydrochloride (DOX) as a model anticancer drug, and their drug loading and encapsulation efficiencies as well as pH‐dependent drug release behavior were investigated. The anticancer activity of the drug‐loaded HNCaps was extensively evaluated using MTT assay against human breast cancer cells (MCF7). The cytotoxicity assay results as well as superior physicochemical and biological features of the fabricated HNCaps mean that the developed DOX‐loaded HNCaps have excellent potential for cancer chemotherapy. © 2020 Society of Chemical Industry     

Dual‐stimuli‐responsive polymer‐coated mesoporous silica nanoparticles used for controlled drug delivery

In this article, a temperature‐ and pH‐responsive delivery system based on block‐copolymer‐capped mesoporous silica nanoparticles (MSNs) is presented. A poly[2‐(diethylamino)ethyl methacrylate)] (PDEAEMA)‐b‐poly(N‐isopropyl acrylamide) (PNIPAM) shell on MSNs was obtained through the surface‐initiated atom transfer radical polymerization. The block copolymer PDEAEMA‐b‐PNIPAM showed both temperature‐ and pH‐responsive properties. The release of the loaded model molecules from PDEAEMA‐b‐PNIPAM‐coated MSNs could be controlled by changes in the temperature or pH value of the medium. The as‐desired drug‐delivery carrier may be applied to biological systems in the future. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 42395.     

pH‐ and temperature‐responsive IPN hydrogels based on soy protein and poly(N‐isopropylacrylamide‐co‐sodium acrylate)

pH‐ and temperature‐responsive interpenetrating polymer network (IPN) hydrogels based on soy protein and poly(N‐isopropylacrylamide‐co‐sodium acrylate) were successfully prepared. The structure and properties of the hydrogels were characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, differential scanning calorimetry, and thermogravimetric analyzer. The equilibrium and dynamic swelling/deswelling behaviors and the drug release properties of the hydrogels responding to pH and/or temperature were also studied in detail. The hydrogels have the porous honeycomb structures, good miscibility and thermal stability, and good pH‐ and temperature‐responsivity. The volume phase transition temperature of the hydrogels is ca. 40°C. Changing the soy protein or crosslinker content could be used to control the swelling behavior and water retention, and the hydrogels have the fastest deswelling rate in pH 1.2 buffer solutions at 45°C. Bovine serum albumin release from the hydrogels has the good pH and temperature dependence. The results show that the proposed IPN hydrogels may have potential applications in the field of biomedical materials such as in drug delivery systems. © 2013 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 39781.     

Dual responsive polymeric bionanocomposite gel beads for controlled drug release systems

Scientists are searching potential solutions for cancer treatments as well as ways to avoid the side effects of anti‐cancer agents, via targeted drug delivery. The aim of this research is to propose dual responsive beads based on sodium alginate (SA), methylcellulose (MC), and magnetic iron oxide nanoparticles (MIONs) for controlled release of 5‐Fluorouracil (5‐FU) as model drug. The beads were prepared by the dual crosslinking of SA and MC in the presence of MIONs. The structural, thermal, morphological, magnetic characteristics as well as the release profile of 5‐FU were studied. The characterization results showed that the drug molecules and MIONs were well dispersed in the polymeric matrix. The cumulative release percentage was ca. 80% at pH = 4.2 and 40% at pH = 7.2 after 6 h. Thus, the sensitivity of beads on the pH value was verified. Moreover, the release profile exhibited reduction with an increase in the concentration of MIONs under an external magnetic field. The obtained results confirmed the dual sensitive release of 5‐FU (i.e., PH/magnetic) that can be used for the targeted and controlled drug delivery systems. © 2017 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2017 , 134, 45143.     

Gum Acacia‐cl‐poly(acrylamide)@carbon nitride Nanocomposite Hydrogel for Adsorption of Ciprofloxacin and its Sustained Release in Artificial Ocular Solution

In the present work, a nanocomposite hydrogel is designed consisting of gum acacia, poly(acrylamide) and carbon nitride by facile microwave approach. This nanocomposite hydrogel is sensitive to environmental stimuli which is essential for its application in environmental remediation and as a drug delivery system. The effects of carbon nitride percentage and microwave Watt variation on swelling capacity of gum acacia‐cl‐poly(acrylamide)@carbon nitride (Ga‐cl‐PAM@C₃N₄) nanocomposite hydrogel are analyzed. The structural characterizations are considered by numerous techniques such as FTIR (Fourier transform infra‐red spectroscopy), X‐ray diffraction, transmission electron microscopy, scanning electron microscopy, and elemental mapping. Batch experiment is performed for remediation of ciprofloxacin (CIP) drug from water. Various parameters such as effect of ciprofloxacin doses, Ga‐cl‐PAM@C₃N₄ nanocomposite hydrogel dosage, pH, time and temperature for adsorption of CIP on gum acacia‐cl‐poly(acrylamide)@carbon nitride nanocomposite hydrogel is examined. Maximum adsorption capacity of Ga‐cl‐PAM@C₃N₄ nanocomposite hydrogel observed is 169.49 mg g^?1 at pH 6.4. The drug loading and drug release capacity of Ga‐cl‐PAM@C₃N₄ nanocomposite hydrogel is investigated for ciprofloxacin. Drug release is monitored in artificial ocular solution (pH 8), saline (pH 5.5), acetate buffer (pH 2.2), and distilled water. Maximum drug release is observed in artificial ocular solution.     

Synthesis and characterization of novel pH‐responsive poly(2‐hydroxylethyl methacrylate‐co‐N‐allylsuccinamic acid) hydrogels for drug delivery

In this study, N‐allylsuccinamic acid (NASA) was synthesized in a single step with a yield of 85%. Carboxylic acid containing NASA was characterized through Fourier transform infrared (FTIR) radiation and ¹H‐NMR and ¹³C‐NMR analysis, and then it was used for synthesis of poly(2‐hydroxylethyl methacrylate‐co‐N‐allylsuccinamic acid) [p(HEMA‐co‐NASA)] hydrogels. The structure of the obtained pH‐responsive p(HEMA‐co‐NASA) hydrogels were characterized with FTIR spectroscopy and scanning electron microscopy analysis, and their swelling characterization was carried out under different drug‐release conditions. In the application step of the study, the hydrogels were used for the in vitro release of vitamin B12 and Rhodamine 6G, which were selected as model drugs. We determined that the hydrogels used as a drug‐delivery matrix could release the drug they had absorbed under different release conditions (phosphate‐buffered saline, 0.9% NaCl, and pH 1.2) at high rates for time periods of up to 24 h. © 2013 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 39660.     

pH-responsive chitosan/sulfobutyl ether-β-cyclodextrin supramolecular nanoparticles for controlled release of sodium ferulate

A pH-responsive supramolecular nanoparticles was constructed through the electrostatic interaction from anionic sulfobutyl ether-β-cyclodextrin (SBE₇-β-CD) and two positively charged chitosan (CS-75% and CS-95%). The prepared nanoparticles were characterized by UV-vis absorption spectra, x-ray diffraction, dynamic light scattering, transmission electron microscopy, and zeta potential. It was found that the CS/SBE₇-β-CD nanoparticles can be disassembly by increasing pH value and reassembled by reducing to the original pH value. To explore the potential of the obtained nanoparticles as a drug delivery vehicle, a negatively charged anticardio cerebrovascular drug sodium ferulate (SF) was loaded. The result indicated that the SF could be efficiently encapsulated in its nanoparticle nucleus under simulated gastric conditions with lower pH (pH 2.0), while effective release is triggered in a simulated intestinal environment with higher pH (pH 8.5). The assembly/disassembly behavior and drug loading/release property make CS/SBE₇-β-CD nanoparticles promising candidates for pH stimulation responsive drug delivery system, which has a broad application prospect in the treatment of cardiovascular and cerebrovascular diseases, diabetes and other chronic diseases.     

Supercritical carbon dioxide–assisted synthesis of stimuli-responsive magnetic poly(N-isopropylacrylamide)–ferrite biocompatible nanocomposites for targeted and controlled drug delivery

Supercritical carbon dioxide–assisted synthesis of poly(N-isopropylacrylamide)–ferrite nanocomposites was carried out by polymerization reaction of N-isopropyl acrylamide monomer in the presence of ferrite nanoparticles. They were characterized by Fourier transform infrared, X-ray diffraction, transmission electron microscopy, atomic force microscopy, and vibrating sample magnetometry analysis. Drug loading and release profiles were studied. Nanomaterials showed pH-dependent drug release profile. Polymer nanocomposites in comparison to ferrite nanoparticles showed impressive drug release activity, with a release percent of 20.98–76.54%, and greater biocompatibility in breast cancer cells, with a cell viability of 81–93%. This pH-dependent drug release activity and magnetic property of polymer nanocomposites can be used for controlled and targeted drug delivery.     

Colon‐specific oral delivery of vitamin B2 from poly(acrylamide‐co‐maleic acid) hydrogels: An in vitro study

Hydrogels, composed of poly(acrylamide‐co‐maleic acid) were synthesized and the release of vitamin B₂ from these gels was studied as a function of the pH of the external media, the initial amount of the drug loaded, and the crosslinking ratio in the polymer matrix. The gels containing 3.8 mg of the drug per gram gel exhibit almost zero‐order release behavior in the external media of pH 7.4 over the time interval of more than their half‐life period (t_1/2). The amount of the drug loaded into the hydrogel also affected the dynamic release of the encapsulated drug. As expected, the gels showed a complete swelling‐dependent mechanism, which was further supported by the similar morphology of the swelling and release profiles of the drug‐loaded sample. The hydrophilic nature of the drug riboflavin does not contribute toward the zero‐order release dynamics of the hydrogel system. On the other hand, the swelling osmotic pressure developed between the gels and the external phase, due to loading of the drug by equilibration of the gels in the alkaline drug solution, plays an effective role in governing the swelling and release profiles. Finally, the minimum release of the drug in the swelling media of pH 2.0 and the maximum release with zero‐order kinetics in the medium of pH 7.4 suggest that the proposed drug‐delivery devices have a significant potential to be used as an oral drug‐delivery system for colon‐specific delivery along the gastrointestinal (GI) tract. © 2002 Wiley Periodicals, Inc. J Appl Polym Sci 84: 1133–1145, 2002; DOI 10.1002/app.10402     

Preparation and characterizations of superparamagnetic iron oxide‐embedded poly(2‐hydroxyethyl methacrylate) nanocarriers

The present study aims at formulating a novel multifunctional biocompatible superparamagnetic nanoparticles carrier system with homogeneously dispersed magnetic material in solid polymer matrix of poly(2‐hydroxyethyl methacrylate) (PHEMA). The nanocomposites were designed by modified suspension polymerization of 2‐hydroxyethyl methacrylate followed by in situ coprecipitation of iron oxide inside the nanoparticle matrix yielding magnetic PHEMA (mPHEMA) nanocomposites. The so prepared nanocomposites were characterized by Fourier transform Infrared spectroscopy, X‐ray diffraction technique, Raman spectroscopy, electron diffraction, and energy‐dispersive X‐ray spectroscopy confirming the presence of Fe₃O₄ inside the PHEMA nanoparticles. The magnetization studies of nanocomposites conducted at room temperature using vibrating sample magnetometer suggested for their superparamagnetic nature having saturation magnetization (Ms) of 20 emu/g at applied magnetic field of 5 kOe. Transmission electron microscopy, field‐emission scanning electron microscopy, and dynamic light scattering/zeta potential measurements were also performed which revealed that size of mPHEMA nanocomposites was lying in the range of 60–300 nm having zeta potential of ?93 mV. The nanocomposites showed no toxicity as revealed by cytotoxicity test performed on L‐929 fibroblast by extract method. The results indicated that the prepared superparamagnetic mPHEMA nanocomposites have enormous potential to provide a possible option for magnetically assisted targeted delivery of anticancer drugs. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 40791.     

Effect of pH on the drug release rate from a new polymer–drug conjugate system

The corresponding N‐hydroximide and N‐methyl‐N‐hydroximide of poly[ethylene‐alt‐(maleic anhydride)] (weight average molecular weight (M_w) of 100–500 g mol^?1) were prepared as a new oral drug delivery system. Syntheses of N‐hydroximide and N‐methylhydroxamic acid of poly[ethylene‐alt‐(maleic anhydride)] were carried out by chemical modification of polymer with hydroxylamine and N‐methylhydroxylamine, respectively, to give water‐soluble polymers. These activated polymers were immobilized with ketoprofen in the presence of dicyclohexylcarbodiimide to give the corresponding water‐insoluble ketoprofen conjugates. All products were characterized by elemental analysis as well as Fourier transform infrared and ¹H NMR spectra. In vitro release of ketoprofen was studied by measuring UV absorption at λ_max = 260 nm as a function of time. This study demonstrated the potential use of N‐hydroximide and N‐methyl‐N‐hydroxamic acid of poly[ethylene‐alt‐(maleic anhydride)] as a drug delivery system. Controlled release was studied at different pH values and at different temperatures. At physiological temperature, the amount of drug released increased with increasing pH. The copolymer‐drug adducts released the drug very slowly at the low pH found in the stomach thus protecting the drug from the action of high acid conditions and resident digestive enzymes. These N‐hydroxamic acid polymer‐drug conjugates were found to be potentially useful in the delivery of macromolecular drugs to targeted sites in the lower gastrointestinal tract and the colon area. Copyright © 2007 Society of Chemical Industry     

Dual‐responsive semi‐interpenetrating network beads based on calcium alginate/poly(N‐isopropylacrylamide)/poly(sodium acrylate) for sustained drug release

To improve the mechanical strength of natural hydrogels and to obtain a sustained drug‐delivery device, temperature‐/pH‐sensitive hydrogel beads composed of calcium alginate (Ca‐alginate) and poly(N‐isopropylacrylamide) (PNIPAAm) were prepared in the presence of poly(sodium acrylate) (PAANa) with ultrahigh molecular weight (M_η ≥ 1.0 × 10⁷) as a strengthening agent. The influence of PAANa content on the properties, including the beads stability, swelling, and drug‐release behaviors, of the hydrogels was evaluated. Scanning electron microscopy and oscillation experiments were used to analyze the structure and mechanical stability of the hydrogel beads, respectively. The results show that stability of the obtained Ca‐alginate/PNIPAAm hydrogel beads strengthened by PAANa the alginate/poly(N‐isopropyl acrylamide) hydrogel bead (SANBs) was significantly improved compared to that of the beads without PAANa (NANBs) at pH 7.4. The swelling behavior and drug‐release capability of the SANBs were markedly dependent on the PAANa content and on the environmental temperature and pH. The bead sample with a higher percentage of PAANa exhibited a lower swelling rate and slower drug release. The drug release profiles from SANBs were further studied in simulated intestinal fluid, and the results demonstrated here suggest that SANBs could serve as a potential candidate for controlled drug delivery in vivo. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011     

In vitro release of rifampicin and biocompatibility of oleoylchitosan nanoparticles

Oleoylchitosan (OCS) self‐assembled nanoparticles as a carrier system for hydrophobic drug delivery was proposed. The OCS nanoparticles were prepared by an o/w emulsification method. Mean diameter of the OCS nanoparticles was around 275.3 nm. All the OCS and OCS nanoparticles have good biocompatibility from the cytotoxicity testing and erythrocyte toxicity assay. And the biocompatibility of OCS nanoparticles was better than OCS. Rifampicin, as a model drug, was investigated for its release properties in vitro. The release of rifampicin from solution with pH 6.0 and 6.8 was characterized by a faster release than from solution with pH 3.8. The increase of sodium tripolyphosphate could slower the release of drug. The sample with low concentration of rifampicin, released faster and entirely. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2009     

Magnetic lamellar nanohydroxyapatite as a novel nanocarrier for controlled delivery of 5-fluorouracil

Magnetic nanoparticles are attractive carriers for drug delivery and layered materials intercalated by drug molecules exhibit improved safety and effectiveness of drug delivery. In this work, we report the loading of a model anticancer drug, 5-fluorouracil (5FU), into a magnetic layered nanohydroxyapatite (ML-HAP) by intercalation technique. The as-prepared ML-HAP nanoparticles with loaded 5FU were characterized using transmission electron microscopy (TEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), and vibrating sample magnetometer. We find that, within a certain drug concentration, the drug molecules can be intercalated into the gallery of ML-HAP without breaking its lamellar structure. The drug loading capacity of ML-HAP is extremely large. The drug release profiles display pH-dependent behavior and the drug release mechanisms are a combination of drug diffusion and HAP dissolution. Furthermore, ML-HAP/5FU shows strong superparamagnetism and good biocompatibility. The ML-HAP can be an efficient platform for targeted anticancer drug delivery.     

Structure–property relationship of pH‐sensitive (PCL)2(PDEA‐b‐PPEGMA)2 micelles: Experiment and DPD simulation

The experiment and dissipative particle dynamics simulation were carried out on four polymers with different block ratios for the investigation of the structure–property relationship of (poly(ε‐caprolactone)₂‐[poly(2‐(diethylamino)ethyl methacrylate)‐b‐poly(poly(ethylene glycol) methyl ether methacrylate)]₂ [(PCL)₂(PDEA‐b‐PPEGMA)₂] micelles. The miktoarm star polymers assembled into spherical micelles composed of PCL core, pH‐sensitive PDEA mesosphere and poly (ethylene glycol) methyl ether methacrylate (PPEGMA) shell. When decreasing pH from 7.4 to 5.0, the hydrodynamic diameter and transmittance of (PCL)₂(PDEA‐b‐PPEGMA)₂ micelles increased along with globule‐uneven‐extended conformational transitions, owing to the protonation of tertiary amine groups of DEA at lower pH conditions. Doxorubicin (DOX) was mainly loaded in the pH‐sensitive layer, and more DOX were loaded in the core when increasing drug concentrations. The in vitro DOX release from the micelles was significantly accelerated by decreasing pH from 7.4 to 5.0. The results demonstrated that the pH‐sensitive micelles could be used as an efficient carrier for hydrophobic anticancer drugs, achieving controlled and sustained drug release. © 2014 American Institute of Chemical Engineers AIChE J, 60: 3634–3646, 2014