Prototype Gastro-Resistant Soft Gelatin Films and Capsules—Imaging and Performance In Vitro

The following study is a continuation of the previous work on preparation of gastro-resistant films by incorporation of cellulose acetate phthalate (CAP) into the soft gelatin film. An extended investigation on the previously described binary Gelatin-CAP and ternary Gelatin-CAP-carrageenan polymer films was performed. The results suggest that the critical feature behind formation of the acid-resistant films is a spinodal decomposition in the film-forming mixture. In the obtained films, upon submersion in an acidic medium, gelatin swells and dissolves, exposing a CAP-based acid-insoluble skeleton, partially coated by a residue of other ingredients. The dissolution-hindering effect appears to be stronger when iota-carrageenan is added to the film-forming mixture. The drug release study performed in enhancer cells confirmed that diclofenac sodium is not released in the acidic medium, however, at pH 6.8 the drug release occurs. The capsules prepared with a simple lab-scale process appear to be resistant to disintegration of the shell structure in acid, although imperfections of the sealing have been noticed.

Download Full-text

Development of Oral Dissolvable Films of Diclofenac Sodium for Osteoarthritis Using Albizia and Khaya Gums as Hydrophilic Film Formers

Journal of Drug Delivery ◽

10.1155/2016/6459280 ◽

2016 ◽

Vol 2016 ◽

pp. 1-11 ◽

Cited By ~ 7

Author(s):

Martina Aduenimaa Bonsu ◽

Kwabena Ofori-Kwakye ◽

Samuel Lugrie Kipo ◽

Mariam El Boakye-Gyasi ◽

Mary-Ann Fosu

Keyword(s):

Drug Release ◽

Diclofenac Sodium ◽

Extraction Yield ◽

Physicomechanical Properties ◽

Drug Diffusion ◽

Ftir Studies ◽

Film Forming ◽

Swelling Capacity ◽

Excipient Compatibility

Oral dissolvable films (ODFs) of diclofenac sodium intended for osteoarthritis were prepared using Albizia and Khaya gums as hydrophilic film formers. The physicochemical properties of the gums were characterized and the gums were used to prepare diclofenac sodium ODFs (~50 mg/4 cm2 film) by solvent casting. The two gums showed satisfactory film forming properties. The physicomechanical properties, drug-excipient compatibility, and in vitro drug release of the films in phosphate buffer pH 6.8 were studied. Khaya gum had higher extraction yield, moisture content, insoluble matter and true density while Albizia gum showed greater swelling capacity, solubility, and minerals content. The ODFs were thin, soft, and flexible with smooth glossy surfaces and possessed satisfactory physicomechanical properties. FTIR studies showed that no interaction occurred between the drug and the gums. The ODFs disintegrated in <45 s achieved >75% drug release within 7 min with dissolution efficiencies of ~83–96%. Drug releases from F2, F3, F4, F5, and F6 were similar to F1 (p>0.05; f1<15 and f2≥50) while F7 differed markedly from F1 (p<0.001; f1>15 and f2<50). Drug release followed the Higuchi kinetic model which is indicative of Fickian drug diffusion.

Download Full-text

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.

Download Full-text

Smart Starch-Gelatin Films Incorporated with Curcumin

Oriental Journal Of Chemistry ◽

10.13005/ojc/360610 ◽

2020 ◽

Vol 36 (6) ◽

pp. 1088-1095

Author(s):

Le Thi Bich Nguyet ◽

Vinh Tien Nguyen

Keyword(s):

Acetic Acid ◽

Food Packaging ◽

Gelatin Film ◽

Film Properties ◽

Elongation At Break ◽

Independent Variables ◽

Gelatin Films ◽

Film Forming ◽

Central Composite Experimental Design ◽

Central Composite

In this study, we developed a starch-gelatin film incorporated with synthesized curcumin to be used as a pH-sensitive smart material for food packaging. The film-forming mixture contained five components: starch, gelatin, glycerol, acetic acid and curcumin. The interactions of the components and their effects on the film properties were investigated by using response surface methodology with central composite experimental design. The results showed impacts of the contents of these components as independent variables on tensile strength, elongation at break, Young’s modulus and solubility of the films. The contents of starch, gelatin and glycerol significantly affect these properties, while acetic acid and curcumin do not (p<0.05). Also, it was shown that the incorporation of curcumin provided the film with the capacity to sense pH changes from neutral to basic (yellow at pH ≤ 8 and orange-red at pH ≥ 9).

Download Full-text

Assessment of a mathematical model considering the effect of flow rate on in-vitro drug-release from PLGA films

E3S Web of Conferences ◽

10.1051/e3sconf/202132104011 ◽

2021 ◽

Vol 321 ◽

pp. 04011

Author(s):

Navideh Abbasnezhad ◽

Farid Bakir ◽

Stéphane Champmartin ◽

Mohammadali Shirinbayan

Keyword(s):

Mathematical Model ◽

Drug Release ◽

Flow Rate ◽

Drug Carrier ◽

Diclofenac Sodium ◽

Drug Eluting Stents ◽

In Vitro Drug Release ◽

Drug Eluting ◽

Release Profiles

Drug-eluting stents implanted in blood vessels are subject to various dynamics of blood flow. In this study, we present the evaluation of a mathematical model considering the effect of flow rate, to simulate the kinetic profiles of drug release (Diclofenac Sodium (DS)) from in-vitro from PLGA films. This model solves a set of non-linear equation for modeling simultaneously the burst, diffusion, swelling and erosion involved in the mechanisms of liberation. The release parameters depending on the flow rate are determined using the corresponding mathematical equations. For the evaluation of the proposed model, test data obtained in our laboratory are used. To quantify DS release from drug-carrier PLGA films, we used the flow-through cell apparatus in a closed-loop. Four flow rate values are applied. For each value, the model-substance liberation kinetics showed an increase in drug released with the flow rate. The simulated release profiles show good agreement with the experimental results. Therefore, the use of this model could provide a practical tool to assess in-vitro drug release profiles from polymer matrices under continuous flow rate constraint, and could help improve the design of drug eluting stents.

Download Full-text

Modulation of Drug Release from Natural Rubber Coated Capsule Loaded with Sodium Bicarbonate and Camphor

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.844.170 ◽

2013 ◽

Vol 844 ◽

pp. 170-173

Author(s):

Thawatchai Phaechamud

Keyword(s):

Drug Release ◽

Sodium Bicarbonate ◽

Natural Rubber ◽

Ammonium Carbonate ◽

Hydrophobic Properties ◽

Film Forming ◽

Hard Gelatin Capsule ◽

Hydrophobic Nature

Natural rubber (NR) has the distinguished film forming and hydrophobic properties. If it could be reformed by an addition of some pore forming agents, the porous topography of this produced material would be interesting for applying in controlled release system. The purpose of this study is to investigate on characterization of film coat and release of propranolol hydrochloride (P) from capsules coated with NR latex. The experimental methods involved the preparation of NR film which was optimally prepared by dipping technique followed by drying onto hard gelatin capsule. The drug release was determined for coated systems fabricated with two different techniques (the dissolving of sodium bicarbonate and the sublimation of ammonium carbonate or camphor). It indicated that ammonium carbonate was incompatible with NR latex. The extent of overall in vitro release of P into HCl buffer pH 1.2 from plain NR film coated capsule at 8 h was approximately 1%. However, the decrease concentration of NR latex or addition of sodium bicarbonate or camphor could enhance the extent of drug release. Scanning electron microscopy (SEM) exhibited the micro porous nature for systems loaded with sodium bicarbonate or camphor. Therefore the hydrophobic nature of NR was proper for sustainable drug release which an incorporation of some poring agent could modulate the release of active compounds.

Download Full-text

DEVELOPMENT AND CHARACTERIZATION OF ORAL SWELLABLE RAPID RELEASE FILM WITH SUPERDISINTEGRANT-SURFACTANT

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2021v13i1.40821 ◽

2021 ◽

pp. 75-80

Author(s):

NEHA IMTIAZ ◽

SUTAPA BISWAS MAJEE ◽

GOPA ROY BISWAS

Keyword(s):

Drug Release ◽

Guar Gum ◽

Diclofenac Sodium ◽

Hydroxypropyl Methylcellulose ◽

Tween 80 ◽

Fickian Diffusion ◽

Disintegration Time ◽

Rapid Release ◽

Oral Films

Objective: Oral disintegrating films consisting of hydrophilic polymer are designed to be quickly hydrated by saliva, adhere to the mucosa and disintegrate rapidly to release the drug. The aim of the present study was to prepare stable, flexible swellable rapid release oral films with hydroxypropyl methylcellulose E15 LV (HPMC) and polyvinyl alcohol (PVA) in different ratios. Guar gum was incorporated as the mucoadhesive agent. In order to achieve rapid disintegration of the film cross carmellose sodium (superdisintegrant) and surfactant like Tween 80 were added. The model drug used in the study was diclofenac sodium. Methods: Films were developed using HPMC E15 LV and PVA by solvent casting method and characterized for thickness, swelling index, disintegration time, folding endurance, drug content, and in vitro drug release pattern and kinetics. Results: The prepared swellable rapid release oral films were quite flexible and transparent with a smooth texture. The swelling index study confirmed that the films possessed the desired swelling property. Fastest disintegration was observed with the oral film containing HPMC: PVA in the ratio of 2:1, guar gum at 120 mg, 20% w/w crosscarmellose sodium and 4%w/w Tween 80. The swellable rapid release oral films were found to follow either Higuchi or Korsmeyer-Peppas model with drug release following either Fickian or non-Fickian diffusion. Maximum drug release of around 70% was observed from the above-mentioned film in 1hr in simulated salivary fluid. Conclusion: Therefore, swellable rapid release oral films with HPMC E15 LV: PVA, guar gum, croscarmellose sodium and Tween 80 demonstrated satisfactory swelling, rapid disintegration and improved drug release for oromucosal absorption.

Download Full-text

DESIGN AND PERFORMANCE VERIFICATION OF NEWLY DEVELOPED DISPOSABLE STATIC DIFFUSION CELL FOR DRUG DIFFUSION/PERMEABILITY STUDIES

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11s2.28506 ◽

2018 ◽

Vol 11 (14) ◽

pp. 1

Author(s):

Ankit Kumar Yadav ◽

Varun Garg ◽

Monica Gulati ◽

Parikshit Bansal ◽

Kompal Bansal ◽

...

Keyword(s):

Diclofenac Sodium ◽

Time Interval ◽

Diffusion Cell ◽

Permeable Membrane ◽

Rigid Frame ◽

Receptor Compartment ◽

Diffusion Studies ◽

And Performance ◽

Permeability Studies

Objectives: The present study describes a disposable static diffusion cell for in vitro diffusion studies to achieve better results as compared to well existing Franz diffusion cell (FDC) in terms of the absence of bubbles, variable receptor compartment, ease of handling, and faster results.Materials and Methods: The cell consists of a cup-shaped donor compartment made of semi permeable that could be either cellophane membrane or, animal skin fitted to a rigid frame, which is supported on a plastic plate that contains a hole for the sample withdrawal. The receptor compartment is a separate unit, and it could be any container up to 500ml volume capacity. The most preferred receptor compartment is glass beaker. In the present study, goatskin was used as semi-permeable membrane and verification of its performance was carried out through diffusion studies using gel formulations of one each of the four-selected biopharmaceutical classification system (BCS) class drugs. Metronidazole, diclofenac sodium, fluconazole, and sulfadiazine were used as model drugs for BCS Class I, II, III, and IV, respectively.Results: The newly developed diffusion cell (NDDC) was found to provide faster and more reproducible results as compared to FDC. At the time interval of 24 h, the cell was found to exhibit a higher diffusion of metronidazole, diclofenac sodium, fluconazole, and sulfadiazine by 0.65, 0.65, 0.32, and 0.81 folds, respectively. The faster release obtained with NDDC was attributed to a larger surface area of skin as compared to that in FDC.Conclusion: It was concluded that better reproducibility of results could be achieved with NDDC.

Download Full-text

PREPARATION AND CHARACTERIZATION OF LAFUTIDINE AS IMMEDIATE RELEASE ORAL STRIP USING DIFFERENT TYPE OF WATER-SOLUBLE POLYMER

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i5.28292 ◽

2018 ◽

Vol 10 (5) ◽

pp. 249 ◽

Cited By ~ 1

Author(s):

Saba Abdulhadee Jabir ◽

Halah Talal Sulaiman

Keyword(s):

Drug Release ◽

Methyl Cellulose ◽

Water Soluble ◽

Low Grade ◽

Disintegration Time ◽

Water Soluble Polymer ◽

Surface Ph ◽

Drug Content ◽

Film Forming

Objective: The objective of the present study was to design and optimize oral fast dissolving film (OFDF) of practically insoluble drug lafutidine in order to enhance bioavailability and patient compliance especially for a geriatric and unconscious patient who are suffering from difficulty in swallowing.Methods: The films were prepared by a solvent casting method using low-grade hydroxyl propyl methyl cellulose (HPMC E5), polyvinyl alcohol (PVA), and sodium carboxymethyl cellulose (SCMC) as film forming polymers. Polyethylene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer to enhance the film forming properties of the polymer. Tween 80 (1% solution) and poloxamer407 were used as a surfactant, citric acid as a saliva stimulating agent, and croscarmellose as a super disintegrant. Films were then tested for both physical (weight variation, thickness, surface pH, drug content) and mechanical (folding endurance, tensile strength, percent elongation, Young's modulus) characteristics. In vitro disintegration, time and drug release profile were also determined for each formula.Results: Films were found to be satisfactory when evaluated for both physical and mechanical characterizations. The surface pH of all the films was found to be within the range of salivary pH 6.8. The USP dissolution apparatus type II (paddle type) was used for in vitro drug release studies. The optimized formulation F13 gave 100 % of drug released at 2 min. It also showed satisfactory surface pH (6.2±0.2), drug content (100.1±0.01%), the disintegration time of (7.0±0.5) seconds and the time needed for 80% of medication to be released (T80%) was 0.96 min.Conclusion: Lafutidine OFDF was formulated using HPMC E5 as film-forming a polymer with PEG400 as a plasticizer. Combination of tween80 (1% solution) and poloxamer407 as a surfactant were used in the presence of croscarmellose as a super disintegrant. The chosen OFDF disintegrates within seven seconds, releases the drug rapidly and gives an action.

Download Full-text

Grewia asiatica Mucilage: A Smart Gelling Polymeric Material for Pharmaceutical Applications In Vitro Studies

Current Materials Science ◽

10.2174/2666145412666191125124644 ◽

2020 ◽

Vol 12 (2) ◽

pp. 117-126

Author(s):

Nitin Gupta ◽

Giriraj T. Kulkarni ◽

Pravin Kumar ◽

Rajendra Awasthi

Keyword(s):

Drug Release ◽

Polymeric Material ◽

Diclofenac Sodium ◽

Skin Irritation ◽

In Vitro Release ◽

Penetration Enhancers ◽

Release Mechanism ◽

Drug Release Profile ◽

Therapeutic Benefits

Background: Natural plant-based materials have several advantages. They are biodegradable, biocompatible, non-toxic, cost-effective, environment friendly, easily available, and can undergo chemical modification. Objective: Grewia asiatica extracts contain various phytoconstituents and have therapeutic benefits such as antimicrobial and anti-diabetic properties. They form colloidal dispersions and make a highly viscous gel in water. Considering these properties of Grewia asiatica mucilage, the present work was aimed to investigate its application in the formulation of gel for the topical delivery of diclofenac sodium. Method: Gel formulations were prepared with and without penetration enhancers using 1% w/w diclofenac sodium as a model drug. The formulations were subjected to different evaluation tests like physical characterization, pH, spreadability, skin irritation, gel retrogradation, drug content and in vitro drug diffusion. The in vitro diffusion of the drug from different formulations was compared with the in vitro drug release profile of the marketed formulation (Omni gel, Cipla, India). To assess the release mechanism, the in vitro release data was analyzed using Korsmeyers-Peppas’ equation. Results: The mucilage showed good gelling behavior in 5.50, 5.75, 6.00, 6.25 and 6.50% concentrations. All the formulations followed the anomalous transport mechanism of drug release. The formulation BP3 showed 90% of drug release after 5.2h of dissolution study, which was similar to the marketed formulation. Hence, formulation BP3 was ideal among all the formulations. Conclusion: It might be concluded that, the Grewia asiatica mucilage may be used as a natural polymeric material for gel formulation.

Download Full-text

Gelatin Films Modified with Acidic and Polyelectrolyte Polymers—Material Selection for Soft Gastroresistant Capsules

Polymers ◽

10.3390/polym11020338 ◽

2019 ◽

Vol 11 (2) ◽

pp. 338 ◽

Cited By ~ 1

Author(s):

Bartosz Maciejewski ◽

Małgorzata Sznitowska

Keyword(s):

Material Selection ◽

Continuous Phase ◽

Gelatin Film ◽

Scanning Calorimetry ◽

Adhesive Properties ◽

Polyelectrolyte Complexes ◽

Gelatin Films ◽

Film Forming ◽

Anionic Polysaccharides ◽

Insoluble Polymers

The following investigation comprised the formation of acid-resistant gelatin-based films, intended for future use in soft-capsule technology. Such film compositions were obtained by including nonionized forms of acid-insoluble polymers in a gelatin-based film-forming mixture. The selected films were additionally modified with small amounts of anionic polysaccharides that have potential to interact with gelatin, forming polyelectrolyte complexes. The obtained film compositions were subjected to, e.g., disintegration tests, adhesiveness tests, differential scanning calorimetry (DSC), and a transparency study. As a result of the performed study, some commercial enteric polymers (acrylates), as well as cellulose acetate phthalate, were selected as components that have the ability to coalesce and form a continuous phase within a gelatin film. The use of a small amount (1.5%) of additional gelling polymers improved the rheological characteristics and adhesive properties of the obtained films, with ί-carrageenan and gellan gum appearing to be the most beneficial.

Download Full-text