Novel mucoadhesive polymer: Synthesis and mucoadhesion of poly[acrylic acid‐co‐poly(ethylene glycol) monomethylether monomethacrylate‐co‐dimethylaminoethyl methacrylate]

This study was to design a mucoadhesive based on the biological and physicochemical properties of the buccal mucosa to achieve optimal mucoadhesion in the aqueous buccal environment. Since the buccal surface is negatively charged, a series of novel mucoadhesive poly[acrylic acid‐co‐poly(ethylene glycol) monomethylether monomethacrylate‐co‐dimethylaminoethyl methacrylate] [poly (AA‐PEGMM‐DMEMA)] were synthesized by incorporating the cationic monomer DMEMA into poly(AA‐PEGMM) to enhance the interactions between the mucohadhesive polymer and the buccal mucosa. The compositions of poly(AA‐PEGMM‐DMEMA) were varied by changing the content of DMEMA from 0 to 4.8 mol % while keeping the mole ratio of AA to PEGMM at a constant 9 : 1. It was found that the force of mucoadhesion of poly(AA‐PEGMM‐DMEMA) increased initially, as DMEMA content increased, and reached the maximum at 1% of DMEMA. Further increasing the content of DMEMA decreased the mucoadhesion. The polymers with 0.5 to 2.9% DMEMA appeared to have maximum mucoadhesion after prehydration for 5 min. An ATR–FTIR spectroscopy study revealed that intrapolymer interactions and intersurface interactions played opposite roles in the mucoadhesion performance of the polymers. Optimal mucoadhesion can be achieved by balancing these two interactions. © 2004 Wiley Periodicals, Inc. J Appl Polym Sci 94:2431–2437, 2004     

Techniques for the Assessment of Mucoadhesion in Drug Delivery Systems: An Overview

Abstract

In recent years mucoadhesive drug delivery systems have been developed for oral, buccal, nasal, ocular, rectal and vaginal routes for either systemic or local effects. Mucoadhesive drug delivery systems are presently being explored because of their potential advantages including increased residence time of the drug at the site of application, relatively rapid uptake of the drug into the systemic circulation, and enhanced bioavailability of the therapeutic agents. This review focuses on trends and techniques for mucoadhesion assessment which includes various experimental methods that have been used for the characterization of mucoadhesive polymers and/or delivery systems. These techniques are categorized into two methods, namely methods for mechanism assessment and methods for formulation evaluation. The techniques used to evaluate mecha nisms of mucoadhesion include atomic force microscopy, texture analysis, rheological, wetting and zeta potential measurements for the assessment of interactions between the mucoadhesive polymer/system and mucosal surface. The methods for the evaluation of mucoadhesion based formulations are also further classified as ex vivo, in vitro as well as pharmacokinetic methods. Hence, the techniques highlight the possibility of evaluating mucoadhesion phenomenon in spite of its complexity.     

Development of pellets of nifedipine using HPMC K15 M and κ-carrageenan as mucoadhesive sustained delivery system and in vitro evaluation

Polymeric mucoadhesive pellets of nifedipine were designed using computer software and they were prepared by extrusion-spheronization using HPMC K15M and κ-carrageenan with microcrystalline cellulose. A randomized rotatable two factor central composite design was applied for assessment of influence of two independent variables such as concentration of κ-carrageenan and HPMC K15M on dependent variables. Pellets were characterized by FTIR, DSC, SEM, flow properties, particle size, abrasion resistance, sphericity, drug content, percent production yield, in vitro drug release, ex vivo mucoadhesion, stability studies and similarity factor. The optimized formulation was selected based on criteria of sphericity nearest to 1.0 with maximum cumulative drug release percentage. Formulation NF6 exhibited sufficient porous spheres, free flowing and smooth surface mucoadhesion of 91.34 % and drug content 98.22 ± 0.37 %. Kinetic modeling revealed that the formulation followed the Higuchi model and showed the Quassi-Fickian drug release mechanism. The similarity factor, F2 value, was found to be 74 ± 6 and there was no significant change in drug content and ex vivo mucoadhesion after 90 days at 40 ± 2 °C, and 75 ± 5 % RH clearly indicated the optimized batch NF6 was stable. Thus, it can be concluded that use of κ-carrageenan, microcrystalline cellulose and HPMC K15M at the 20:35:10 w/w ratio could provide an effective carrier for enhancement of sphericity and sustained release of matrix pellets.     

Spray-dried Cefixime Encapsulated Poly(lactide-co-glycolide) Microparticles: Characterization and Evaluation of In Vitro Release Kinetics with Antibacterial Activity

Our study reports on the development of novel biodegradable microparticles prepared by a spray-drying technique using the poly(lactide-co-glycolide) (PLGA), a biodegradable polymer for the controlled delivery of cefixime. Cefixime is a water-soluble drug having short biological half-life of 3 h. The behavior of PLGA in controlling drug release responses of cefixime microparticles was investigated. The resultant microparticles were characterized by scanning electron microscopy, encapsulation efficiency, particle-size distribution, X-ray diffraction, and in vitro dissolution studies (pH 7.2). To investigate the type of release mechanism that occurs, dissolution data were plotted according to different kinetic models. The in vitro release profiles from microparticles followed first order and Higuchi model release. Antibacterial studies were carried out using a standard agar diffusion method to determine the effectiveness of formulations in inhibiting the growth of microorganisms. It showed that the released drug from the formulations was effectively inhibiting the growth of microorganisms with the minimum inhibitory concentration of < 1 µg/mL. Data revealed the potential of formulations for treatment of infections caused by various microorganisms. Thus, this study demonstrates the high potential of the spray-drying technique to obtain stable cefixime microparticles with good encapsulation efficiency to achieve a delivery profile that would yield the controlled released level of the drug over a long period of time (74 h).     

Sweet Potato Starch Microparticles as Controlled Drug Release Carriers: Preparation and In Vitro Drug Release

The aim of this study was to investigate the in vitro drug release behavior of sweet potato starch (SPS) microparticles intended for controlled drug delivery applications. Diclofenac sodium (DS) was used as a model drug candidate in the present study. SPS microparticles were prepared using a spray-drying technique by varying the polymer concentration and drug loading. The mean particles size of drug-loaded spray-dried SPS microparticles was between 10.3 and 13.1 µm. The mean particle size increased slightly with increase in the concentration of SPS. The mean particle size of spray-dried SPS microparticles increased from 10.3 to 13.1 µm when the concentration of SPS increased from 2 to 4% w/v. Under the current spray-drying conditions, the percentage yield of spray-dried SPS microparticles did not vary much among the various formulations and it was between 65.2 and 70.1%. The encapsulation efficiencies of SPS microparticles formulations was between 95.1–98.2%, suggesting good encapsulating ability of the SPS polymer by spary drying. Drug release from all the formulations of spray-dried SPS microparticles was controlled over period of 6 h. The cumulative amount of drug release from the spray-dried SPS microparticles decreased with an increase in the concentration of SPS, while it increases as the drug loading is increased. Release of the drug from spray-dried SPS microparticles followed Fick's law of diffusion since a good correlation coefficient (R²) was observed with the Higuchi plots (R² = 0.9928 to 0.9979).     

Thiolated chitosans: In vitro comparison of mucoadhesive properties

The aim of this study was to compare the mucoadhesive properties of thiolated chitosans with regard to their molecular mass and type of immobilized thiol ligand. Mediated by a carbodiimide, aromatic‐ and aliphatic‐thiol‐bearing compounds were covalently attached to low‐ and medium‐molecular‐mass chitosan. All synthesized conjugates displayed on average 320 ± 50 μmol of immobilized free thiol groups per gram of polymer. The rheological synergy was observed by the mixture of equal volumes of polymer with mucin solution. Because of the increase in viscosity of the conjugate/mucin mixture, the self‐crosslinking properties and the interaction of thiomers with the mucus layer could be confirmed. Further mucoadhesion of the chitosan conjugates was evaluated in vitro with the rotating cylinder method and tensile studies on excised porcine intestinal mucosa. The results show a significantly enhanced residence time (p < 0.05) on the mucosa of all thiolated chitosans compared to the unmodified polymer. Among all of the conjugates tested, the following rank order of mucoadhesion could be determined: Chitosan–thiobutylamidine > Chitosan–4‐mercaptobenzoic acid > Chitosan–glutathione > Chitosan–6‐mercaptonicotinic acid > Chitosan–N‐acetyl cysteine > Chitosan–thioglycolic acid > Unmodified chitosan. The charge, pK_a, and reactivity of the attached compounds were found to be important factors influencing the mucoadhesive potential of the polymer. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011     

Tamarind Seed Polysaccharide-g-Poly(N-Vinyl-2-Pyrrolidone): Microwave-Assisted Synthesis,Characterization, and Evaluation as Mucoadhesive Polymer

Graft copolymer of N-vinyl-2-pyrrolidone and tamarind seed polysaccharide was prepared using microwave assisted graft copolymerization and evaluated for mucoadhesive applications. Graft copolymerization was optimized using response surface methodology employing microwave power and exposure time as the independent variables, and grafting efficiency as the response variable. The buccal patches of metronidazole formulated using the graft copolymer showed ex vivo bioadhesion time of 9.3 h with >80% of the drug getting released while the buccal patches formulated using tamarind seed polysaccharide showed ex vivo bioadhesion time of 5 h releasing only 50% of the drug.     

Chemometric analysis of selective polyphenolic groups in Asparagus racemosus (Shatavar) root extracts by traditional and supercritical fluid (CO2) based extractions

ABSTRACT

Asparagus racemosus root extracts were prepared by supercritical fluid (CO₂), soxhlet, and maceration-based methods also with various pretreatments. Thereafter, these root extracts were analyzed by High-Performance Liquid Chromatography, along with the chemometric study of the disparate phenolic groups. Among these, supercritical fluid (CO₂) based extract has a larger number of polar compounds and the antioxidant activity (98.54 ± 0.22 µM Trolox equivalent mg^?1). It also has the best cell viability (94.37 ± 1.12%) and insulin release (0.82 ± 1.12 ng mL^?1) on β-pancreatic RINm-5F cells whereas, the best extractive yield (75.80 ± 3.44% w/w) was observed for pretreated aqueous soxhlet-based extract.     

Possible Mechanism of Inhibition of 6-Methoxy-Benzoxazolin-2(3H)-One on Germination of Cress (Lepidium sativum L.)

6-Methoxy-benzoxazolin-2(3H)-one (MBOA) inhibited the germination of cress (Lepidium sativum L.) seeds at concentrations greater than 0.03 mM. Inhibition was overcome by sucrose, suggesting that MBOA may inhibit sugar metabolism in cress seeds. Induction of α-amylase activity in seeds was also inhibited by MBOA at concentrations greater than 0.03 mM. Inhibition of both germination and induction of α-amylase activity increased with increasing concentrations of MBOA, and the extent of germination correlated positively with the activity of α-amylase in the seeds. MBOA added to a reaction mixture for α-amylase assay did not affect enzyme activity, indicating that MBOA does not inhibit in vitro α-amylase activity. Cress seeds germinated approximately 16 hr after incubation, and inhibition of α-amylase by MBOA occurred within 6 hr after incubation. These results suggest that MBOA may inhibit the germination of cress seeds by inhibiting the induction of α-amylase activity, because α-amylase plays a key role in the conversion of reserve carbohydrate into soluble sugars, a prerequisite for seed germination.     

QUANTIFICATION OF GALLIC ACID AND ELLAGIC ACID FROM THE SEED OF CORNUS OFFICINALIS BY UHPLC METHOD AND THEIR ANTIOXIDANT ACTIVITY

Gallic acid and ellagic acid have been identified in the seed of Cornus officinalis by the use of an ultrahigh performance liquid chromatography (UHPLC) method coupled with a diode array detector (DAD). The water extract of C. officinalis seed contained the highest gallic acid content (3.03 ± 0.10 mg/g seed), which was followed by aqueous methanol extract (2.43 ± 0.10 mg/g seed) and aqueous ethanol extract (1.53 ± 0.25 mg/g seed). But a higher concentration (12.32 ± 0.45 mg/g seed) of ellagic acid was obtained from extraction with aqueous methanol than with aqueous ethanol (11.03 ± 0.42 mg/g seed) and water (7.28 ± 0.16 mg/g seed). After heat treatment and acid hydrolysis, C. officinalis seed had higher concentrations of gallic acid and ellagic acid, contributing to more potent antioxidant activity. The results demonstrated a rich source of gallic acid and ellagic acid in C. officinalis seed, which might provide a novel source of these natural antioxidants.     

Preparation and characterization of miglitol-loaded Poly (d,l-lactide-co-glycolide) microparticles using high pressure homogenization-solvent evaporation method

Sustained release Miglitol-loaded poly (d, l-lactide-co-glycolide) (PLGA) microparticles were prepared using high pressure homogenization-solvent evaporation method. 2³ full factorial design was employed to study effect of independent variables (X₁-Polymer amount; X₂-Surfactant concentration and X₃-Homogenization Pressure) on percent encapsulation efficiency (%EE) as response. The microparticles produced were characterized for particle size, morphology, % EE, drug polymer compatibility and in vitro drug release. An average particle size of Miglitol-loaded PLGA microparticles was 230.1?nm and found almost spherical with smooth surface. % EE ranged from 58.7%?±?2.11 to 86.5%?±?0.24 depending on the polymer amount, surfactant concentration and homogenization pressure. An absence of chemical interaction between drug-polymer and reduction in % crystallinity of drug was confirmed by FTIR and X-ray diffraction analysis respectively. In vitro release studies showed a sustained release of Miglitol from microparticles up to 12?hrs.     

Adhesion of conventional and self-adhesive resin cements to indirect resin composite using different surface conditioning methods

This study evaluated the adhesion of conventional and self-adhesive resin cements to indirect resin composite (IRC) using different surface conditioning methods. Cylindrical IRC specimens (N = 192) were randomly assigned to four surface conditioning methods (n = 8 per group): (a) Control group, (b) Hydrofluoric acid, (c) Tribochemical silica-coating, and (d) 50 μm Al₂O₃ air-abrasion. Specimen surfaces were finished using silicon carbide papers up to 600 grit under water irrigation, rinsed and dried. Direct composite blocks were bonded to IRC specimens using three conventional resin cements (Multilink, Panavia F2.0, and Resicem) and three self-adhesive resin cements (RelyX U100, Gcem, Speed Cem). Specimens were subjected to shear bond strength test in a Universal Testing Machine (0.5 mm/min). Failure types were categorized as mixed, adhesive and cohesive. Data were analyzed using 2-way ANOVA and Tukey’s tests. Two-parameter Weibull modulus, scale (m) and shape (0) were calculated. The bond strength results (MPa) were significantly affected by the surface conditioning method (p < 0.0001) and cement type (p < 0.001). For Panavia F2.0, Resicem, air-abrasion with 50 μm Al₂O₃ significantly increased the results (22.6 ± 6.5, 26.2 ± 6.5, respectively) compared to other conditioning methods (13.6 ± 1.4–21.9 ± 3.1) but for Multilink, hydrofluoric acid etching (20.5 ± 3.5) showed significantly higher results (p < 0.01). For the self-adhesive resin cements, air-abrasion with 50 μm Al₂O₃ significantly increased the results compared to other conditioning methods, except for RelyX U100 (p < 0.05). After air-abrasion with Al₂O₃, Gcem, (11.64), RelyX U100 (9.05), and SpeedCem (8.29) presented higher Weilbul moduli. Exclusively cohesive failure in the IRC was observed with RelyX U100 and Speedcem after Al₂O₃ air-abrasion.     

Self-Assembled,Chitosan Grafted PLGA Nanoparticles for Intranasal Delivery: Design,Development and Ex Vivo Characterization

The objective of present study was to modify the surface of Poly(D,L-lactide-co-glycolide acid) (PLGA) nanoparticles (NPs) with chitosan to enhance the mucoadhesive potential of carrier system. Grafting of chitosan on PLGA surface was carried out via amide bond formation mediated by carbodiimide and confirmed by FTIR spectroscopy. Self-assembled PLGA NPs containing chlorpromazine hydrochloride were fabricated by 2³ factorial design. The improved mucoadhesive potential was confirmed by several tests including in vitro mucoadhesion study. Ex vivo permeation was satisfactory. Histopathological study on sheep nasal mucosa revealed safe mucoadhesion. They were also found to be robust on accelerated stability study.     

Thermophysical properties of laboratory-prepared corn/wheat dried distillers grains and dried distillers solubles dehydrated with superheated steam and hot air

The objective of this study was to dry–wet distillers grains and centrifuged solubles and to examine the effect of two different drying media, superheated steam and hot air, at different drying temperatures (110, 130, and 160°C), moisture contents (5–30% wb), and percentages of solubles’ presence (0 or 100%) on some thermophysical properties of laboratory-prepared corn/wheat dried distillers co-products, including geometric mean diameter (d_g), particle density (ρ_p), bulk density (ρ_b), bulk porosity (?_b), specific heat (C), effective thermal diffusivity (α_eff), and bulk thermal conductivity (λ_b). The values of d_g of corn/wheat dried distillers co-products ranged from 0.358 ± 0.001 to 0.449 ± 0.001 mm. Experimental values of ρ_p, ρ_b, and ?_b varied from 1171 ± 6 to 1269 ± 3 kg m^?3, from 359 ± 7 to 605 ± 5 kg m^?3, and from 0.54 ± 0.01 to 0.71 ± 0.01 kg m^?3, respectively. The values of α_eff were between 0.58 × 10^?7 and 0.93 × 10^?7 m² s^?1. The calculated values of C ranged from 1887 ± 11 to 2599 ± 19 J kg^?1 K^?1, and the values of λ_b of corn/wheat dried distillers co-products ranged from 0.06 ± 0.01 to 0.09 ± 0.01 W m^?1 K^?1. Multiple linear regression prediction models were developed to predict the changes in d_g, ρ_p, ρ_b, ?_b, C, α_eff, and λ_b of laboratory-prepared corn/wheat dried distillers co-products with different operational factors.     

Bioadhesive hydrophobic chitosan microparticles for oral delivery of insulin: In vitro characterization and in vivo uptake studies

Hydrophobically modified polymeric matrices for drug delivery were developed by N‐acylation of chitosan with long(C₁₈) and medium chain(C₈) fatty acid chlorides like octanoyl and oleoyl chloride. Chemical modifications of chitosan were confirmed by IR spectra and trinitrobenzenesulphonic acid assay. Modified chitosan particles were prepared by ionotropic gelation with sodium tripolyphosphate. Hydrophobic modification was confirmed by contact angle measurements. Scanning electron micrographs showed the presence of compact microparticles. Swelling studies showed that oleoyl chitosan exhibited low swelling profile than octanoyl chitosan at acidic pH. In vitro release profile at pH 7.4 showed that about 90% of insulin was released by 5th hour. ELISA studies proved that the microparticles were capable of maintaining biological activity of insulin. Mucoadhesion studies proved that oleoyl derivative was more mucoadhesive than octanoyl derivative. In vivo uptake studies of fluorescent‐labeled microparticles on rat intestinal sections showed that oleoyl chitosan microparticles exhibited significant uptake than octanoyl chitosan. These results suggests that oleoyl moiety would resist degradation by the gastric enzymes and will enhance mucoadhesivity through hydrophobic interactions and also the permeability by loosening the tight junctions, thus making it a useful carrier for oral peptide delivery applications. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010     

Development,In Vitro and In Vivo Evaluation of pH Responsive β-CD-Comethacrylic Acid-Crosslinked Polymeric Microparticulate System for Solubility Enhancement of Rosuvastatin Calcium

Current research work was conducted for enhancing solubility of rosuvastatin calcium. A highly stable, biocompatible, and nontoxic β-cyclodextrin-g-poly(methacrylic acid) graft polymeric network was developed. Formulations proved entrapment efficacy (%) in between 82.30?±?0.25 and 89.00?±?0.25 and gel fraction between 90.34?±?1.012 and 95.25?±?1.331. Formulation HM2 had shown optimum swelling and drug release, i.e., 85.74% at pH 6.8. The best-fit model was first-order kinetics with anomalous diffusion as release mechanism. Likewise, solubility enhancement, i.e., 9.59-folds was determined at pH 6.8. It was concluded that hydrogel microparticles are the promising tools for improving solubility and bioavailability of hydrophobic drugs.     

Separation of Radiogallium from Zinc Using Membrane-Based Liquid-Liquid Extraction in Flow: Experimental and COSMO-RS Studies

ABSTRACT

A switch from batch to continuous manufacturing of gallium-68 (⁶⁸Ga) and ⁶⁸Ga-labeled pharmaceuticals can be advantageous, as it recycles isotopically-enriched zinc-68 (⁶⁸Zn), removes pre- and post-irradiation target manipulations, and provides scalability via dose-on-demand production. Herein we report efficient extraction of radiogallium (^66,67,68Ga = *Ga) from ZnCl₂/HCl solutions in batch and in flow using a membrane-based liquid-liquid separator. From 5.6 M ZnCl₂/3 M HCl, a 1/2 (v/v) diisopropyl ether (ⁱPr₂O)/trifluorotoluene (TFT) solvent extracts 76.3 ± 1.9% of *Ga and 1.9 ± 1.6% of Zn in flow using a single pass through. From 1 M ZnCl₂/6 M HCl, a 1/2 (v/v) n-butyl methyl ether (n-BuOMe)/TFT solvent extracts 95.7 ± 2.0% of *Ga and 0.005 ± 0.003% of Zn in flow. TFT plays a key role in controlling the interfacial tension between the aqueous and the organic phases, ensuring clean membrane-based separation. The process did not extract Cu, Mn, and Co but did extract Fe. Using HGaCl₄ and ZnCl₂ as the extractable species, the COSMO-RS theory predicts the solvation-driven extraction of Ga and Zn with a mean unsigned error of prediction of 4.0% and 3.4% respectively.     

Microencapsulation of Ketoprofen in Blends of Acrylic Resins by Spray Drying

Microparticles of ketoprofen entrapped in blends of acrylic resins (Eudragit RL 30D and RS 30D) were successfully produced by spray drying. The effects of the proportion ketoprofen : polymer (1:1 and 1:3) and of spray-drying parameters (drying gas inlet temperatures of 80 and 100°C; microencapsulating composition feed flow rates of 4 and 6 g/min) on the microparticles properties (drug content, encapsulation efficiency, mean particle size, moisture content, and dissolution behavior) were evaluated. Differential scanning calorimetry (DSC) thermograms and X-ray diffractograms of the spray-dried product, the free drug, and the physical mixture between the free drug and spray-dried composition (blank) were carried out. Microparticles obtained at inlet temperature of 80°C, feed flow rate of 4 g/min, and ketoprofen : acrylic resin ratio of 1:3 presented an encapsulation efficiency of 88.1%, moisture content of 5.8%, production yield around 50%, and a higher reduction in dissolution rate of the entrapped ketoprofen. Sigmoidal shape dissolution profiles were presented by the spray-dried microparticles. The dissolution profiles were relatively well described by the Weibull model, a showing high coefficient of determination, R ², and a mean absolute error between experimental and estimated values of between 4.6 and 10.1%.     

Characterization and Benzo[a]pyrene Content Analysis of Camellia Seed Oil Extracted by a Novel Subcritical Fluid Extraction

A novel continuous subcritical n‐butane extraction technique for Camellia seed oil was explored. The fatty acid composition, physicochemical properties, and benzo[a]pyrene content of Camellia seed oil extracted using this subcritical technique were analyzed. Orthogonal experiment design (L₉(3⁴)) was adopted to optimize extraction conditions. At a temperature of 45 °C, a pressure of 0.5 MPa, a time of 50 min and a bulk density of 0.7 kg/L, an extraction yield of 99.12 ± 0.20 % was obtained. The major components of Camellia seed oil are oleic acid (73.12 ± 0.40 %), palmitic acid (10.38 ± 0.05 %), and linoleic acid (9.15 ± 0.03 %). Unsaturated fatty acids represent 83.78 ± 0.03 % of the total fatty acids present. Eight physicochemical indexes were assayed, namely, iodine value (83.00 ± 0.21 g I/100 g), saponification value (154.81 ± 2.00 mg KOH/g), freezing‐point (?8.00 ± 0.10 °C), unsaponifiable matter (5.00 ± 0.40 g/kg), smoke point (215.00 ± 1.00 °C), acid value (1.24 ± 0.03 mg KOH/g), refrigeration test (transparent, at 0 °C for 5.5 h), and refractive index (1.46 ± 0.06, at 25 °C). Benzo[a]pyrene was not detected in Camellia seed oil extracted by continuous subcritical n‐butane extraction. In comparison, the benzo[a]pyrene levels of crude Camellia seed oil extracted by hot press extraction and refined Camellia seed oil were measured at 26.55 ± 0.70 and 5.69 ± 0.04 μg/kg respectively.     

Arabinoxylan-Based Mucoadhesive Oral Films of Tizanidine HCL Designed and Optimized Using Central Composite Rotatable Design

In the current study, a natural pharmaceutical excipient, arabinoxylan, was extracted from ispaghula husk and used to develop controlled release of mucoadhesive oral films of tizanidine hydrochloride. Film formulations were designed and optimized by central composite rotatable design, selecting arabinoxylan (X₁) and glycerol (X₂) as variables. Prepared films were evaluated for chemical compatibility of the ingredients, surface morphology, mechanical strength, in vitro drug release, ex vivo drug permeation and ex vivo mucoadhesion strength. Results revealed that selected ingredients were compatible and quite capable of producing films with desired characteristics.