APPLICATION OF SYNTHETIC AND NATURAL POLYMERS IN PREPARATION AND CHARACTERIZATION OF DOMPERIDONE FAST-DISSOLVING FILMS

Objective: The present research work is mainly focused on solubility enhancement of domperidone which is a biopharmaceutical classification system Class II drug using natural and synthetic polymers. Methods: The solubility was enhanced by the kneading method with the drug: polymer (1:0.5, 1:0.75, and 1:1) using β-cyclodextrin. The fast dissolving films (FDFs) of domperidone were prepared by incorporating the solid dispersion (SD) SDK3 by solvent casting method using hydroxypropyl methylcellulose K15 M (HPMC) and gellan gum in various concentrations for preparing FDFs. Various pre- and post-compression parameters, drug and excipients compatibility studies were evaluated by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction analysis (XRD). Results: The maximum drug release of 98.86 % was achieved within 30 min for 1:1 ratio of solid dispersion using β-cyclodextrin, was optimized and taken for further development of FDFs. From the in vitro drug release studies films prepared with 10% w/w of HPMC K 15 (FH5) and 10% w/w of gellan gum (FG5) showed enhanced dissolution rate compared to other formulations. The formulation FHG with combination of polymers, namely, HPMC K 15 and gellan gum in 1:1 ratio showed drug release of 97.22% within 15 min only when compared with the optimized formulations. FTIR and DSC studies revealed that there were no interactions between drug and excipients. XRD studies revealed slight conversion of crystalline form to amorphous. The optimized formulation FHG found to be stable under accelerated stability studies. Conclusions: The polymers in combination are a potential candidate for use in the formulation of FDF.

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Fabrication and In Vitro Evaluation of pH-Sensitive Polymeric Hydrogels as Controlled Release Carriers

Gels ◽

10.3390/gels7030110 ◽

2021 ◽

Vol 7 (3) ◽

pp. 110

Author(s):

Muhammad Suhail ◽

Chih-Wun Fang ◽

Arshad Khan ◽

Muhammad Usman Minhas ◽

Pao-Chu Wu

Keyword(s):

Controlled Release ◽

Drug Release ◽

Acrylic Acid ◽

Chondroitin Sulfate ◽

Diclofenac Sodium ◽

Research Work ◽

Controlled Delivery ◽

Scanning Calorimetry ◽

Release Studies

The purpose of the current investigation was to develop chondroitin sulfate/carbopol-co-poly(acrylic acid) (CS/CBP-co-PAA) hydrogels for controlled delivery of diclofenac sodium (DS). Different concentrations of polymers chondroitin sulfate (CS), carbopol 934 (CBP), and monomer acrylic acid (AA) were cross-linked by ethylene glycol dimethylacrylate (EGDMA) in the presence of ammonium peroxodisulfate (APS) (initiator). The fabricated hydrogels were characterized for further experiments. Characterizations such as Scanning electron microscopy (SEM), Thermogravimetric analysis (TGA), Differential scanning calorimetry (DSC), Powder X-ray diffractometry (PXRD), and Fourier transform infrared spectroscopy (FTIR) were conducted to understand the surface morphology, thermodynamic stability, crystallinity of the drug, ingredients, and developed hydrogels. The swelling and drug release studies were conducted at two different pH mediums (pH 1.2 and 7.4), and pH-dependent swelling and drug release was shown due to the presence of functional groups of both polymers and monomers; hence, greater swelling and drug release was observed at the higher pH (pH 7.4). The percent drug release of the developed system and commercially available product cataflam was compared and high controlled release of the drug from the developed system was observed at both low and high pH. The mechanism of drug release from the hydrogels followed Korsmeyer–Peppas model. Conclusively, the current research work demonstrated that the prepared hydrogel could be considered as a suitable candidate for controlled delivery of diclofenac sodium.

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EFFECT OF POLYMERS ON THE PHYSICOCHEMICAL AND DRUG RELEASE PROPERTIES OF TRANSDERMAL PATCHES OF ATENOLOL

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i4.24916 ◽

2018 ◽

Vol 10 (4) ◽

pp. 68

Author(s):

Manish Kumar ◽

Vishal Trivedi ◽

Ajay Kumar Shukla ◽

Suresh Kumar Dev

Keyword(s):

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Research Work ◽

High Moisture ◽

Transdermal Drug Delivery System ◽

Permeable Membrane ◽

Transdermal Patches ◽

Egg Membrane ◽

Hydrophilicity And Hydrophobicity

Objective: The objective of this research work was to develop a transdermal drug delivery system containing atenolol with different ratios of hydrophilic and hydrophobic polymeric combinations, using solvent evaporation technique and to examine the effect of hydrophilicity and hydrophobicity of polymers on the physicochemical and drug release properties of transdermal patches.Methods: Solvent casting method has been used to formulate transdermal patches. Hydroxypropyl methylcellulose (HPMC), Polyvinylpyrrolidone (PVP), Ethylcellulose (EC) in different combination ratios were used as the polymer. Propylene glycol was used as a plasticizer. Permeation enhancers such as span 80 were used to enhance permeation through the skin. In vitro diffusion study was carried out by franz diffusion cell using egg membrane as a semi-permeable membrane for diffusion.Results: Result showed that the thickness of the all batch of patches varied from 0.32 to 0.39 mm with uniformity of thickness in each formulation. Formulations F1 to F3 had high moisture content varied from 2.07±0.09 to 2.56±0.15 and high moisture uptake value varied from 3.21±0.35 to 4.09±0.38, due to a higher concentration of hydrophilic polymers. Drug content of all batches was ranged between 85.92±1.32 to 95.71±1.42. Folding endurance values off all batches were more than 75. Formulation batches F1 to F3 showed higher cumulative drug release varied from 61.34% to 68.11% as compared to formulation batches F4 to F6.Conclusion: Higher proportion of hydrophilic polymer in the formulation of transdermal patches, gives higher percentage drug release from prepared patches. The finding of the study indicates that hydrophilicity and hydrophobicity of polymer effects the physicochemical and drug release properties of transdermal patches and an optimum proportion of hydrophilic and hydrophobic polymer is required for the preparation of effective transdermal patches.

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Formulation and investigation of crushed puffed rice-chitosan-HPMC based polymeric blends as carrier for sustained stomach specific drug delivery of piroxicam using 3(2) Taguchi mathematical design studies

International Current Pharmaceutical Journal ◽

10.3329/icpj.v6i11.36435 ◽

2018 ◽

Vol 6 (11) ◽

pp. 61-80 ◽

Cited By ~ 1

Author(s):

Shashank Soni ◽

Veerma Ram ◽

Anurag Verma

Keyword(s):

Drug Release ◽

Release Kinetics ◽

Drug Loading ◽

Hydroxypropyl Methylcellulose ◽

Research Work ◽

Pharmaceutical Journal ◽

Weight Variation ◽

Zero Order Release ◽

Puffed Rice

In the present experimental investigation an attempt has been made to assess the utility of Crushed Puffed Rice (CPR)-High Molecular Weight Chitosan (HMWCH)-Hydroxypropyl Methylcellulose K15M (HPMC K15M) as a polymeric carrier for the sustained stomach delivery of Piroxicam (PRX). A total of nine formulations were prepared by using 3 (2) Taguchi factorial design, physically blending drug and polymer(s) followed by encapsulation into hard gelatin capsules size 1. The prepared capsules were evaluated for various performance such as weight variation, drug contents, in vitro buoyancy and drug release in 0.1 M HCl. The effect of drug loading on in vitro performance of the formulations was also determined. Crushed puffed rice (CPR) remained buoyant for up to average time span of 06 hr as an unwetted irregular mass in 0.1 M HCl. However, when combined with HMWCH or HPMC K15M or HPMC K15M + HMWCH a low -density cylindrical raft type hydrogel was formed which remained buoyant for up to 12 hr and released up to 99% drug in a sustained manner from 8 to 12 hr following zero order release kinetics. It was also observed that drug release from drug + CPR matrices followed Fickian mechanism. Combination of CPR + HMWCH or HMWCH + HPMC K15M also follows Fickian mechanism. Obtained data from the research work suggests that CPR in combination with HMWCH or HPMC K15M or HPMC has sufficient potential to be used as a carrier for stomach specific delivery of gastric irritant drug like PRX.Soni et al., International Current Pharmaceutical Journal, April 2018, 6(11): 61-80http://www.icpjonline.com/documents/Vol6Issue11/01.pdf

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Development and In-Vitro Evaluation of pH Responsive Polymeric Nano Hydrogel Carrier System for Gastro-Protective Delivery of Naproxen Sodium

Advances in Polymer Technology ◽

10.1155/2019/6090965 ◽

2019 ◽

Vol 2019 ◽

pp. 1-13

Author(s):

Rai Muhammad Sarfraz ◽

Muhammad Rouf Akram ◽

Muhammad Rizwan Ali ◽

Asif Mahmood ◽

Muhammad Usman Khan ◽

...

Keyword(s):

Drug Release ◽

Naproxen Sodium ◽

Research Work ◽

Entrapment Efficiency ◽

Gravimetric Analysis ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Swelling Behaviour ◽

X Ray

Current research work was carried out for gastro-protective delivery of naproxen sodium. Polyethylene glycol-g-poly (methacrylic acid) nanogels was developed through free radical polymerization technique. Formulation was characterized for swelling behaviour, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), and Thermal Gravimetric Analysis (TGA), Powder X-ray diffraction (PXRD), Zeta size distribution, and Zeta potential measurements, and in-vitro drug release. pH dependent swelling was observed with maximum drug release at higher pH. PXRD studies confirmed the conversion of loaded drug from crystalline to amorphous form while Zeta size measurement showed size reduction. On the basis of these results it was concluded that prepared nanogels proved an effective tool for gastro-protective delivery of naproxen sodium.

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DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE MICROSPHERE-LOADED INTRANASAL GEL OF VENLAFAXINE HYDROCHLORIDE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2016.v9s3.13057 ◽

2016 ◽

Vol 9 (9) ◽

pp. 139

Author(s):

Kritika Saikia ◽

Bhupen Kalita ◽

Banasmita Kalita

Keyword(s):

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Entrapment Efficiency ◽

Sustained Drug Release ◽

Scanning Calorimetry ◽

Venlafaxine Hydrochloride ◽

Gel Formulations ◽

Carbopol 934P ◽

Mucoadhesive Microsphere

ABSTRACTObjective: The main objective of the present work is to develop and characterize a novel mucoadhesive intranasal microsphere gel formulation ofdrug venlafaxine to control the drug release through nasal mucosa and reach the target site with minimal side effect. The objectives of the studyare (1) formulation of mucoadhesive microspheres, (2) evaluation of mucoadhesive microspheres, (3) formulation of mucoadhesive microsphereloadednasal gel, (4) and evaluation of nasal gel.Methods: Preparation of chitosan microsphere: The chitosan microspheres were prepared by emulsion cross-linking method. Preparation ofmicrosphere-loaded gel: The nasal gels with varying concentrations of Carbopol 934P were prepared by dispersing required quantity of Carbopol inrequired quantity of distilled water with continuous stirring and kept overnight for complete hydration. The gel was then modified by the addition ofvarying proportion of hydroxypropyl methylcellulose (HPMC) K4M.Results: The prepared microspheres were evaluated for size distribution, surface morphology by scanning electron microscopy, entrapment efficiency,compatibility by Fourier transform infrared spectroscopy, and differential scanning calorimetry. Entrapment efficiency of all formulations was foundmore than 70%. Microsphere formulation containing drug and polymer in the ratio of 1:2.5 was found to be optimized. Optimized microsphereformulation was then incorporated in gel prepared using Carbopol 934P and HPMC. Prepared gel formulations were studied for viscosity, spreadability,and in-vitro drug release in simulated nasal conditions. Viscosity of the optimized batch of gel was recorded at 1056 centipoise. Drug release wasprolonged for the microsphere-in-gel formulations compared to the microspheres alone. For the optimized batch of gel, cumulative drug release of85.67% was found after 8 hrs.Conclusion: The results suggest that venlafaxine hydrochloride mucoadhesive microsphere-loaded nasal gel would give sustained drug release andsuperior bioavailability in the brain sites.Keywords: Venlafaxine, Chitosan, Mucoadhesive, Microsphere, Nasal gel.

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Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model

Pharmaceutics ◽

10.3390/pharmaceutics13050627 ◽

2021 ◽

Vol 13 (5) ◽

pp. 627

Author(s):

Ahmad A. Shahba ◽

Ahmad Y. Tashish ◽

Fars K. Alanazi ◽

Mohsin Kazi

Keyword(s):

Drug Release ◽

Solid Dispersion ◽

Negative Impact ◽

Drug Dissolution ◽

In Vitro Dissolution ◽

Scanning Calorimetry ◽

Dissolution Model ◽

Dissolution Efficiency ◽

Drug Free

The study aims to design a novel combination of drug-free solid self-nanoemulsifying drug delivery systems (S-SNEDDS) + solid dispersion (SD) to enhance cinnarizine (CN) dissolution at high pH environment caused by hypochlorhydria/achlorhydria. Drug-loaded and drug-free liquid SNEDDS were solidified using Neusilin® US2 at 1:1 and 1:2 ratios. Various CN-SDs were prepared using freeze drying and microwave technologies. The developed SDs were characterized by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). In-vitro dissolution studies were conducted to evaluate CN formulations at pH 6.8. Drug-free S-SNEDDSs showed acceptable self-emulsification and powder flow properties. DSC and XRD showed that CN was successfully amorphized into SDs. The combination of drug-free S-SNEDDS + pure CN showed negligible drug dissolution due to poor CN migration into the formed nanoemulsion droplets. CN-SDs and drug-loaded S-SNEDDS showed only 4% and 23% dissolution efficiency (DE) while (drug-free S-SNEDDS + FD-SD) combination showed 880% and 160% enhancement of total drug release compared to uncombined SD and drug-loaded S-SNEDDS, respectively. (Drug-free S-SNEDDS + SD) combination offer a potential approach to overcome the negative impact of hypochlorhydria/achlorhydria on drug absorption by enhancing dissolution at elevated pH environments. In addition, the systems minimize the adverse effect of adsorbent on drug release.

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FORMULATION AND CHARACTERIZATION OF SUSTAINED RELEASE TABLET USING MARDI GUM

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2021.v14i5.41138 ◽

2021 ◽

pp. 52-55

Author(s):

MANGESH M KUMARE ◽

GIRIDHAR R SHENDARKAR

Keyword(s):

Drug Release ◽

Sustained Release ◽

Hydroxypropyl Methylcellulose ◽

Research Work ◽

Release Mechanism ◽

In Vitro Drug Release ◽

Sustained Release Tablet ◽

Weight Variation ◽

Release Tablet

Objective: The present research work was to develop and evaluate alprazolam sustained release tablet using Mardi gum, a comparative study on binding properties of gum and hydroxypropyl methylcellulose (HPMC) was performed. Methods: Formulation of alprazolam tablets (f1–f6) was done by direct compression method using 15%, 30%, and 45% concentration of gum as a natural binder, and HPMC was used as synthetic matrix forming agent. Microcrystalline cellulose was used as diluents, talc, and magnesium stearate as a lubricant and PVP K30 as the binder. The formulated batches were evaluated for parameters such as tablet thickness, % friability, hardness, weight variation, and in vitro drug release characteristics. The release information was fitted into different dynamics models to decide the release mechanism of the drug. Results: The results showed that all the parameters of the developed tablets (f1–f6) were in fulfillment with pharmacopeia limits. In vitro, drug release studies showed that formulation f1 had most controlled and sustained manner releaser with maximum drug release of 97.89±0.52% in 18 h with comparison to f2–f4 and f6 drug release is 98.12±0.55%, 97.24±0.57%, 98.16±0.74%, and 97.26±0.35%, respectively, in 16 h and f5 giving 97.89±0.85% release in 14 h. Conclusion: On the basis of obtained result, it can be concluded that Mardi gum can be used to sustain the drug release as a natural polymer in tablet dosage form.

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Amalgamation of Solid Dispersion and Melt Adsorption Techniques For Augmentation of Oral Bioavailability of Novel Anticoagulant Rivaroxaban

10.21203/rs.3.rs-997661/v1 ◽

2021 ◽

Author(s):

Pranav Shah ◽

Milan Patel ◽

Jigar Shah ◽

Anroop Nair ◽

Sabna Kotta ◽

...

Keyword(s):

Drug Release ◽

Solid Dispersion ◽

Oral Bioavailability ◽

Drug Dissolution ◽

Commercial Application ◽

Scanning Calorimetry ◽

Cytotoxicity Studies ◽

Time Required ◽

Saturated Solubility

Abstract The objective of the present study was to evaluate the potential of solid dispersion adsorbate to improve the solubility and bioavailability of rivaroxaban (RXN). Solid dispersion adsorbate (SDA) of RXN was developed by fusion method using PEG 4000 as carrier and Neusilin as adsorbent. A 32 full factorial design was utilized to formulate various SDAs. The selected independent variables were amount of carrier (X1) and amount of adsorbate (X2). The responses measured were time required for 85% drug release (Y1) and saturated solubility (Y2). MTT assay was employed for cytotoxicity studies on Caco-2 cells. In vivo pharmacokinetics and pharmacodynamic evaluations were carried out to assess the prepared SDA. Pre-compression evaluation of SDA suggests the prepared batches (B1-B9) possess adequate flow properties and could be used for compression of tablets. Differential scanning calorimetry and X-ray diffraction data signified the conversion of crystalline form of drug to amorphous form, a key parameter accountable for improvement in drug dissolution. Optimization data suggests that the amount of carrier and amount of adsorbate significantly (P < 0.05) influence both dependent variables (time required for 85% drug release and saturated solubility). Post-compression data signifies that the compressibility behavior of prepared tablets were within the official standard limits. Significant increase (P < 0.0001) in the in vitro dissolution characteristics of RXN was noticed in optimized SDA (>85% in 10 min) as compared to pure drug, marketed product and directly compressible tablet. Cytotoxicity studies confirm nontoxicity of prepared RXN SDA tablets. Higher Cmax and AUC achieved with RXN SDA tablets indicated enhancement in oral bioavailability (~3 folds higher than the RXN suspension). Higher bleeding time and percentage of platelet aggregation noticed with RXN SDA tablets further substantiate the efficacy of the prepared formulation. In summary, the results showed the potential of RXN SDA tablets to enhance the bioavailability of RXN and hence can be an alternate approach of solid dosage form for its development for commercial application.

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Biopharmaceutical and Pharmacodynamic Characteri-stics of Telmisartan Oral Disintegrating Films

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2019.12.2.6 ◽

2019 ◽

Vol 12 (2) ◽

pp. 4489-4496

Author(s):

Rajesh Kaza ◽

Sujatha Kumari M ◽

Kishore Babu M ◽

Avinash A ◽

Nagaraju R

Keyword(s):

Drug Release ◽

Solid Dispersion ◽

Guar Gum ◽

Research Work ◽

Weight Ratio ◽

Drug Dissolution ◽

Content Uniformity ◽

Natural Polymers ◽

Weight Variation ◽

Forming Characteristics

This research work was aimed to develop the telmisartan fast dissolving films. Fast dissolving films allow rapid drug dissolution in the oral cavity and thereby bypass the first pass metabolism. Solid dispersions of telmisartan using natural polymers such as hupu gum (HG), guar gum (GG) and xanthan gum (XG) were prepared by kneading technique and the optimized solid dispersion was exploited in the development of rapidly dissolving film. Telmisartan films were prepared by solvent casting method using different grades of HPMC (E5, 50 cps and K4M). Six formulations (FT1-FT6) of telmisartan films were prepared and evaluated for their physical characteristics such as thickness, tensile strength, percentage elongation, weight variation, folding endurance, drug content uniformity and surface pH and gave satisfactory results. The compatibility of the drug in the formulation was confirmed by FTIR and DSC studies. The formulations were subjected to disintegration, in vitro drug release and pharmacodynamic studies on spontaneous hypertensive rats (SHR). Amongst the formulations of FT1-FT6, FT6 was found as best formulation which contains HPMC E5 and telmisartan solid dispersion with guar gum at weight ratio of 1:2 and showed excellent film forming characteristics such as disintegration time at 42 sec and percentage drug release 97.98% within 10 minutes. The optimized film formulation (FT6) showed excellent stability over 45 days when stored at 40°C/60% RH. The pharmacodynamic study in SHR proved that fast dissolving films of telmisartan produced a faster onset of action.

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Fast Dissolving Sublingual Strips: A Novel Approach for the Delivery of Isosorbide Dinitrate

Pharmaceutical Sciences ◽

10.15171/ps.2019.34 ◽

2019 ◽

Vol 25 (4) ◽

pp. 311-318

Author(s):

Marzieh Fathei ◽

Mitra Alami-milani ◽

Sara Salatin ◽

Sharahm Sattari ◽

Hassan Montazam ◽

...

Keyword(s):

Drug Release ◽

Isosorbide Dinitrate ◽

Moisture Absorption ◽

Ex Vivo ◽

Hydroxypropyl Methylcellulose ◽

Drug Bioavailability ◽

Scanning Calorimetry ◽

Surface Ph ◽

Drug Content

Background: Isosorbide dinitrate (ISDN) is used for treating the angina attacks. In addition, oral ISDN is available in immediate and sustained release formulations and the bioavailability of ISDN is about 20-25% when taken orally. Further, the ISDN films are developed for sublingual drug delivery by improving drug bioavailability. The present study aimed to design and evaluate the physicochemical properties of the film formulation for sublingual delivery of ISDN. Methods: In the present study, sublingual films were prepared by the solvent casting technique using the hydroxypropyl methylcellulose (HPMC) polymers (i.e., 100, 150 and 200 mg) with a different drug to polymer ratios (i.e., 1:5, 1:7.5 and 1:10). Then, ISDN was evaluated for the film appearance, drug content, surface pH, mucoadhesion force, differential scanning calorimetry (DSC), in vitro drug release, and ex vivo permeability. Results: Based on the results, F3 formulation (1:10 ISDN to HPMC ratio) showed acceptable thickness (0.93 mm), weight (11.14 mg), surface pH (7.82), moisture absorption capacity (6.08%), elasticity (>200), mucoadhesion force (18.05 N/cm2), and drug content (6.22%). Furthermore, the results demonstrated that HPMC polymer improved the characteristics of the films, modified the bioadhesiveness, and finally, enhanced elasticity. However, DSC thermogram failed to show any crystalline drug substance in the films except for F1 (immediate release) and the endothermic peak of ISDN was absent in F2 and F3 films. Therefore, the drug which was entrapped into the film was in an amorphous or disturbed-crystalline phase of the molecular dispersion or dissolved in the melted polymer in the polymeric matrix. Moreover, the drug release from the films was faster compared to the tablet® (P<0.05). Conclusion: In general, the formulation of F1 was observed to be an appropriate candidate for developing the sublingual film for the remedial use.

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