DESIGN AND EVALUATION OF CHITOSAN-HPMC POLYMERIC FILMS FOR TRANSDERMAL DELIVERY OF CAPTOPRIL

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (06) ◽  
pp. 69-72
Author(s):  
Rajesh Sreedharan Nair ◽  
Manickam Balamurugan ◽  
Meng Sheng Teng
Keyword(s):  
Transdermal Delivery ◽  
Moisture Absorption ◽  
Hydroxypropyl Methylcellulose ◽  
Physicochemical Characterization ◽  
Scanning Calorimetry ◽  
Drug Permeation ◽  
Evaporation Technique ◽  
Model Drug ◽  
The Stability

Drug permeation through the skin layers remains a major challenge in transdermal drug delivery. In this study, the permeation enhancing property of chitosan together with its rate-controlling property has been utilized in the development of an efficient transdermal delivery system, using captopril as a model drug. Chitosan-hydroxypropyl methylcellulose (HPMC) films were developed by solvent evaporation technique. The films were characterized for appearance, thickness, weight uniformity, drug content, folding endurance and moisture absorption. Drug-polymer interaction was assessed using ATR-FTIR spectroscopy and Differential Scanning Calorimetry. The in vitro permeation carried out in Franz-type diffusion cells using synthetic Strat-M® membrane, demonstrated that the film coded F2 (Chitosan:HPMC = 50:50) showed a significant increase in drug permeation than F1 (Chitosan:HPMC = 90:10) with a flux value 86.7 µg/cm2/h. The physicochemical characterization and the stability studies confirmed that the formulated films were chemically and physically stable.

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

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.

scholarly journals Influence of Lactobacillus Biosurfactants on Skin Permeation of Hydrocortisone

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 820
Author(s):  
Angela Abruzzo ◽  
Carola Parolin ◽  
Elisa Corazza ◽  
Barbara Giordani ◽  
Massimiliano Pio di Cagno ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Aqueous Solubility ◽  
Skin Hydration ◽  
Permeation Enhancers ◽  
Scanning Calorimetry ◽  
Drug Permeation ◽  
Diffusion Studies ◽  
Model Drug ◽  
Dsc Curves

One of the most widely used strategies to improve drug diffusion through the skin is the use of permeation enhancers. The aim of this work was to investigate the effect of two biosurfactants (BS), produced by Lactobacillus crispatus BC1 and Lactobacillus gasseri BC9, on the skin permeation profile of hydrocortisone (HC, model drug). HC aqueous solubility and in vitro diffusion studies through porcine skin were performed in the presence of BC1-BS and BC9-BS at concentrations below and above critical micellar concentrations (CMC). Moreover, skin hydration tests and differential scanning calorimetry (DSC) analysis were performed to further investigate BS interaction with the outermost layer of the skin. Both BS increased HC solubility, especially at concentrations above their CMC. At concentrations below the CMC, drug permeation through the skin was improved, as the result of a dual effect: a) the formation of a superficial lipophilic environment, as confirmed by the reduction in skin hydration and b) the interaction between BS and the stratum corneum (SC), as demonstrated by the DSC curves. From the obtained data, it appears that BC1-BS and BC9-BS could represent new promising green excipients for drug permeation enhancement through the skin.

scholarly journals FORMULATION AND EVALUATION OF ANTIPARKINSON’S DRUG INCORPORATED TRANSDERMAL FILMS

2019 ◽  
pp. 147-151
Author(s):  
POREDDY SRIKANTH REDDY ◽  
ALAGARSAMY V ◽  
SUBHAH CHANDRA BOSE P ◽  
DAMINENI SARITA ◽  
SRUTHI V
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Physicochemical Characterization ◽  
Molecular Size ◽  
Log P ◽  
Target Drug ◽  
Weight Variation ◽  
Elimination Half ◽  
The Stability ◽  
Transdermal Film

Objective: Ropinirole suitable for transdermal delivery due to its small molecular size (260.37 g/mol), optimum log p (2.3), and low oral bioavailability (50%) due to first-pass metabolism, the short elimination half-life of 4–6 h. Dose of drug is 6 mg/day. Hence, in the present study, an attempt was made to deliver antiparkinson’s drug through transdermal route in the form of transdermal film to attain sustained release using different concentration of drug, polymers stabilizers. Methods: Among the different formulations of matrix type (F1 to F5), F2 and F4 formulations were optimized based on crystallinity. These formulations were carried out for in vitro permeation studies. Out of these two formulations, F4 formulation showed target drug release. Results and Discussion: The formulation F4 containing 2 mg drug, 600 mg hydroxypropyl methylcellulose E15 and 50 mg of Eudragit RS 100 was selected as optimized formulation, after considering its microscopic examination throughout stability, % drug content (98.4%), drug permeated through the cellophane membrane at the end of 72 h, and evaluation of physicochemical characterization parameters such as thickness, weight variation, flatness, folding endurance, moisture content, and tensile strength. Conclusion: The results of physicochemical characterization were ensured the stability of the films. The drug permeation profile was also found to follow Higuchi kinetic model.

3 (2) Factorial Design Assisted Crushed Puffed Rice-HPMC-Chitosan based Hydrodynamically Balanced System of Metoprolol Succinate

2020 ◽  
Vol 10 (3) ◽  
pp. 237-249
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Batch Size ◽  
Metoprolol Succinate ◽  
Zero Order Kinetics ◽  
Two Factors ◽  
Puffed Rice ◽  
Model Drug

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.

scholarly journals DESIGN, FORMULATION, AND CHARACTERIZATION OF APREMILAST-SACCHARIN COCRYSTALS LOADED WITH TOPICAL GEL

2020 ◽  
pp. 60-67
Author(s):  
TEJASWINI MANE ◽  
MUKESH MOHITE
Keyword(s):  
Physicochemical Properties ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Gelling Agent ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Scanning Calorimetry ◽  
Topical Gel ◽  
Solubility Study

Objective: Most of the drugs are relevant to BSC class II and class IV having solubility problems. Cocrystallization of drug with conformer is an immense approach used to explore the physicochemical properties of drug. The objective of the present work was to design formulate and evaluate the drug cocrystals of poorly soluble drug apremilast (APR) with saccharin. Methods: Cocrystals of APR were prepared using the solvent evaporation technique. The saturated solubility study and in vitro dissolution study of cocrystals were carried out. The prepared cocrystals were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-transform infrared (FTIR) spectroscopy. The topical gel of APR cocrystals was formulated optimized and evaluated using three-level factorial design. Results: The cocrystals of APR were prepared in 1:1 molar ratio with saccharin. APR cocrystals showed the improvement in solubility and dissolution as compared to pure APR. The formation of cocrystals was confirmed from change in endothermic peak of DSC and from shifting of FTIR spectra of cocrystals. Crystallinity of cocrystal was confirmed from XRD pattern and noteworthy change in 2θ values of the intense peak. The topical gel of APR cocrystals was formulated and optimized using three-level factorial design using Carbapol-940 and hydroxypropyl methylcellulose (HPMC) as a gelling agent. Conclusion: The cocrystals with altered physicochemical properties of APR were prepared with saccharin and formulated as a topical gel to overcome the problems related to oral administration.

scholarly journals Inclusion Complexes of β and HPβ-Cyclodextrin with α, β Amyrin and In Vitro Anti-Inflammatory Activity

Biomolecules ◽  
2019 ◽  
Vol 9 (6) ◽  
pp. 241 ◽  
Author(s):  
Walter Ferreira da Silva Júnior ◽  
Danielle Lima Bezerra de Menezes ◽  
Luana Carvalho de Oliveira ◽  
Letícia Scherer Koester ◽  
Patrícia Danielle Oliveira de Almeida ◽  
...  
Keyword(s):  
Inclusion Complexes ◽  
Biological Activities ◽  
Physicochemical Characterization ◽  
Inflammatory Activity ◽  
Scanning Calorimetry ◽  
Promising Alternative ◽  
Wide Range ◽  
Natural Mixture ◽  
Anti Inflammatory

α, β amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has a wide range of biological activities. ABAM is isolated from the species of the Burseraceae family, in which the species Protium is commonly found in the Amazon region of Brazil. The aim of this work was to develop inclusion complexes (ICs) of ABAM and β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) by physical mixing (PM) and kneading (KN) methods. Interactions between ABAM and the CD’s as well as the formation of ICs were confirmed by physicochemical characterization in the solid state by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC). Physicochemical characterization indicated the formation of ICs with both βCD and HPβCD. Such ICs were able to induce changes in the physicochemical properties of ABAM. In addition, the formation of ICs with cyclodextrins showed to be an effective and promising alternative to enhance the anti-inflammatory activity and safety of ABAM.

scholarly journals Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 183
Author(s):  
Chen ◽  
Yin ◽  
Ma ◽  
Tu ◽  
Shen
Keyword(s):  
Acute Toxicity ◽  
Hydroxypropyl Methylcellulose ◽  
Sodium Hyaluronate ◽  
Drug Formulation ◽  
Resonance Spectroscopy ◽  
Eye Drops ◽  
Scanning Calorimetry ◽  
Eye Irritation

Azithromycin (AZI) eye drops containing sodium hyaluronate (SH) were developed to improve the bioavailability of AZI. Interaction between AZI and SH in the AZI-SH formulation was investigated by differential scanning calorimetry, X-ray diffraction, and 1H-nuclear magnetic resonance spectroscopy analyses. Moreover, advantages of using SH as an excipient were investigated by comparing physiological properties and pharmacokinetic behaviors of SH-containing AZI eye drops with that of hydroxypropyl methylcellulose (HPMC)-containing formulation. In addition, safety of the developed AZI-SH eye drops was evaluated by in vitro 3-(4,5-dimethyl-2-Thiazyl)-2, 5-diphenyl-2H-tetrazolium bromide assay (MTT assay) and neutral red uptake assay as well as in vivo eye irritation test and acute toxicity test. The results indicated that AZI formed a complex with SH under a slightly acidic condition. The area under the curve (AUC) of AZI in SH-containing formulation was 1.58-fold higher (P<0.01) than that in HPMC-containing formulation due to the interaction between the amine group of AZI and the carboxyl group of SH, despite of the higher viscosity of HPMC-containing formulation. Safety evaluation showed that AZI-SH eye drops caused no obvious eye irritation and acute toxicity. In conclusion, the developed SH-containing AZI formulation possessing advantages of longer retention time and higher drug availability was a promising drug formulation for topical ocular therapy.

scholarly journals PREPARATION, CHARACTERIZATION AND EVALUATION OF FLOATING MICROPARTICLES OF CIPROFLOXACIN

2016 ◽  
Vol 9 (1) ◽  
pp. 1 ◽  
Author(s):  
Sumit Durgapal ◽  
Sayantan Mukhopadhyay ◽  
Laxmi Goswami
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Evaluation Parameters

Objective: The main purpose of this study is to prepare a floating micro articulated drug delivery system of ciprofloxacin by using non-aqueous solvent evaporation technique to increase the bioavailability and therapeutic effectiveness of the drug by prolonging its gastric residence time.Methods: Floating microparticles were prepared by using different low-density polymers such as ethyl cellulose and hydroxypropyl methylcellulose either alone or in combination with the aid of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as percentage yield, drug content, drug entrapment, rheological studies, floating characteristics and in vitro drug release studies.Results: Drug-excipient compatibility studies performed with the help of FTIR instrument indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique is a suitable technique for the preparation of floating microspheres as most of the formulations were discrete and spherical in shape with a good yield of 65% to 85% and 15 to 22 h of floating duration with 90% of maximum percentage floating capacity shown by formulation FM9. Though, different drug-polymer ratios, as well as a combination of polymers, play a significant role in the variation of overall characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, drug content, drug entrapment, rheological studies and in vitro drug release characteristics formulation FM9 was found to fulfil the criteria of ideal floating drug delivery system.Conclusion: Floating microparticles were successfully prepared, and from this study, it can be concluded that the developed floating microspheres of ciprofloxacin can be used for prolonged drug release in the stomach to improve the bioavailability and patient compliance.

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

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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