scholarly journals EFFECT OF POLYMERIC BLEND ON EX-VIVO PERMEATION STUDIES OF ACECLOFENAC LOADED FILM FORMING GEL

Author(s):  
HIMANI BAJAJ ◽  
VINOD SINGH ◽  
RANJIT SINGH ◽  
TIRATH KUMAR

Objective: To date, film-forming systems have been intensively investigated for transdermal drug delivery. Film-forming systems offers various advantages compared over conventional transdermal drug delivery systems. The objective of the present study was to study the effect of polymeric blend on ex-vivo permeation studies of topical film-forming gel of aceclofenac. Methods: Film-forming gels were prepared by using Hydroxypropyl methylcellulose and Eudragit polymeric blend in varied concentrations, polyethylene glycol 400 as plasticizer, ethanol as solvent and tween 80 as a penetration enhancer. The prepared film-forming gels were evaluated and the influence of the concentration and ratio of polymeric blends used plasticizer and ethanol were investigated. Results: All the prepared film-forming gels showed satisfactory properties regarding homogeneity, compatibility, viscosity and pH value. Variation in the concentration of polymers showed a variable effect on drug permeation rate from film-forming gels. Almost, all formulations permeated up to 80% of drug in 12 h and formulation F1 showed a maximum release about 97.54 % in 12 h. Conclusion: Film-forming gels of aceclofenac with sustained-release profile were successfully developed and may provide a promising effective formulation which may improve patient compliance.

2020 ◽  
Vol 10 (3) ◽  
pp. 185-196
Author(s):  
Sudha B. Patil ◽  
Syed Z. Inamdar ◽  
Kakarla R. Reddy ◽  
Anjanapura V. Raghu ◽  
Krishnamachari G. Akamanchi ◽  
...  

Background and Objectives: To develop electro-sensitive transdermal drug delivery systems (ETDDS) using polyacrylamide-grafted-pectin (PAAm-g-PCT) copolymer hydrogel for rivastigmine delivery. Methods: Free radical polymerization and alkaline hydrolysis technique was employed to synthesize PAAm-g-PCT copolymer hydrogel. The PAAm-g-PCT copolymeric hydrogel was used as a reservoir and cross-linked blend films of PCT and poly(vinyl alcohol) as rate-controlling membranes (RCMs) to prepare ETDDS. Results: The pH of the hydrogel reservoir was found to be in the range of 6.81 to 6.93 and drug content was 89.05 to 96.29%. The thickness of RCMs was in the range of 51 to 99 μ and RCMs showed permeability behavior against water vapors. There was a reduction in the water vapor transmission rate as the glutaraldehyde (GA) concentration was increased. The drug permeation rate from the ETDDS was enhanced under the influence of electric stimulus against the absence of an electric stimulus. The increase in flux by 1.5 fold was recorded with applied electric stimulus. The reduction in drug permeability observed when the concentration of GA was increased. Whereas, the permeability of the drug was augmented as an electric current was changed from 2 to 8 mA. The pulsatile drug release under “on– off” cycle of electric stimulus witnessed a faster drug release under ‘on’ condition and it was slow under ‘off’ condition. The alteration in skin composition after electrical stimulation was confirmed through histopathology studies. Conclusion: The PAAm-g-PCT copolymer hydrogel is a useful carrier for transdermal drug delivery activated by an electric signal to provide on-demand release of rivastigmine.


2021 ◽  
Vol 14 ◽  
Author(s):  
Sarbjot Kaur ◽  
Ujjwal Nautiyal ◽  
Pooja A. Chawla ◽  
Viney Chawla

Background: Background: Olanzapine belongs to a new class of dual spectrum antipsychotic agents. It is known to show promise in managing both the positive and negative symptoms of schizophrenia. Drug delivery systems based on nanostructured lipid carriers (NLC) are expected to provide rapid nose-to-brain transport of this drug and improved distribution into and within the brain. Objective: The present study deals with the preparation and evaluation of olanzapine loaded NLC via the intranasal route for schizophrenia. Methods: Olanzapine-NLC were formulated through the solvent injection method using isopropyl alcohol as the solvent, stearic acid as solid lipid, and oleic acid as liquid lipid, chitosan as a coating agent, and Poloxamer 407 as a surfactant. NLC were characterized for particle size, polydispersity index, entrapment efficiency, pH, viscosity, X-ray diffraction studies, in-vitro mucoadhesion study, in- vitro release and ex-vivo permeation studies. The shape and surface morphology of the prepared NLC was determined through transmission electron microscopy. To detect the interaction of the drug with carriers, compatibility studies were also carried out. Results: Average size and polydispersity index of developed formulation S6 was 227.0±6.3 nm and 0.460 respectively. The encapsulation efficiency of formulation S6 was found to be 87.25 %. The pH, viscosity, in-vitro mucoadhesion study, and in- vitro release of optimized olanzapine loaded NLC were recorded as 5.7 ± 0.05, 78 centipoise, 15±2 min, and 91.96 % respectively. In ex-vivo permeation studies, the percent drug permeated after 210 min was found to be 84.03%. Conclusion: These results reveal potential application of novel olanzapine-NLC in intranasal drug delivery system for treatment of schizophrenia.


2020 ◽  
Vol 21 (7) ◽  
Author(s):  
Amanda F. Silva-Alvarez ◽  
Maíra P. Ferreira ◽  
Fabiana T. M. C. Vicentini ◽  
Vinicius Pedrazzi ◽  
Osvaldo de Freitas

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (06) ◽  
pp. 68-70
Author(s):  
Himani Bajaj ◽  
◽  
Vinod Singh ◽  
Ranjit Singh ◽  
Tirath Kumar ◽  
...  

The objective of the present study was to prepare a topical film-forming gel of aceclofenac for the treatment of rheumatic diseases, using a safe and effective drug delivery approach. Aceclofenac film-forming gels were prepared using hydroxypropyl methyl cellulose and chitosan polymeric blend in varying concentrations, polyethylene glycol 400 (PEG 400) as a plasticizer, Tween 80 as a permeation enhancer and ethanol as solvent. The prepared film-forming gels were evaluated and the influence of the concentration and ratio of polymeric blends, plasticizer, and ethanol used were investigated. All the prepared film-forming gels showed satisfactory properties regarding consistency, spreadability and thickness. Variation in the concentration of polymers, ethanol and PEG 400 showed a variable effect on drying time from film-forming gels. Film-forming gels of aceclofenac were successfully developed and may provide a promising effective formulation that may improve patient compliance.


2020 ◽  
Vol 19 (5) ◽  
pp. 360-373 ◽  
Author(s):  
Panoraia I. Siafaka ◽  
Ece Ö. Bülbül ◽  
Gökce Mutlu ◽  
Mehmet E. Okur ◽  
Ioannis D. Karantas ◽  
...  

Alzheimer's disease is a neuropathological disease with symptoms such as language problems, confusion as to place or time, loss of interest in activities, which were previously enjoyed, behavioral changes, and memory loss. Alzheimer's disease and other types of dementia affect almost 46.8 million people globally and are estimated to strike about 131.5 million people in 2050. It has been reported that Alzheimer's is the sixth main cause of mortality. The most used drugs, which are currently approved by the Food, and Drug Administration for Alzheimer’s disease are donepezil, rivastigmine, galantamine, memantine, and the combination of donepezil and memantine. However, most of the drugs present various adverse effects. Recently, the transdermal drug delivery route has gained increasing attention as an emerging tool for Alzheimer's disease management. Besides, transdermal drug delivery systems seem to provide hope for the management of various diseases, due to the advantages that they offer in comparison with oral dosage forms. Herein, the current advancements in transdermal studies with potent features to achieve better Alzheimer's disease management are presented. Many researchers have shown that the transdermal systems provide higher efficiency since the first-pass hepatic metabolism effect can be avoided and a prolonged drug release rate can be achieved. In summary, the transdermal administration of Alzheimer's drugs is an interesting and promising topic, which should be further elaborated and studied.


2017 ◽  
Vol 7 (1) ◽  
pp. 48-53
Author(s):  
Mohd. Yasir ◽  
Dinesh Puri ◽  
S. Kumar ◽  
Krishna Sharma ◽  
Shikha Mishra ◽  
...  

2020 ◽  
Vol 10 ◽  
Author(s):  
Divya Thakur ◽  
Gurpreet Kaur ◽  
Sheetu Wadhwa ◽  
Ashana Puri

Background: Metronidazole (MTZ) is an anti-oxidant and anti-inflammatory agent with beneficial therapeutic properties. The hydrophilic nature of molecule limits its penetration across the skin. Existing commercial formulations have limitations of inadequate drug concentration present at target site, which requires frequent administration and poor patient compliance. Objective: The aim of current study was to develop and evaluate water in oil microemulsion of Metronidazole with higher skin retention for treatment of inflammatory skin disorders. Methods: Pseudo ternary phase diagrams were used in order to select the appropriate ratio of surfactant and co-surfactant and identify the microemulsion area. The selected formulation consisted of Capmul MCM as oil, Tween 20 and Span 20 as surfactant and co-surfactant, respectively, and water. The formulation was characterized and evaluated for stability, Ex vivo permeation studies and in vivo anti-inflammatory effect (carrageenan induced rat paw edema, air pouch model), anti-psoriatic activity (mouse-tail test). Results: The particle size analyses revealed average diameter and polydispersity index of selected formulation to be 16 nm and 0.373, respectively. The results of ex vivo permeation studies showed statistically higher mean cumulative amount of MTZ retained in rat skin from microemulsion i.e. 21.90 ± 1.92 μg/cm2 which was 6.65 times higher as compared to Marketed gel (Metrogyl gel®) with 3.29 ± 0.11 μg/cm2 (p<0.05). The results of in vivo studies suggested the microemulsion based formulation of MTZ to be similar in efficacy to Metrogyl gel®. Conclusion: Research suggests efficacy of the developed MTZ loaded microemulsion in treatment of chronic skin inflammatory disorders.


2019 ◽  
Vol 3 (1) ◽  
pp. 64-74 ◽  
Author(s):  
Ravindra P. Birajdar ◽  
Sudha S. Patil ◽  
Vijaykumar V. Alange ◽  
Raghavendra V. Kulkarni

Objective: The study aimed to prepare electrically-triggered transdermal drug delivery systems (ETDS) using electrically responsive polyacrylamide-graft-gaur gum (PAAm-g-GaG) copolymer. Methods: The PAAm-g-GaG copolymer was synthesized by adopting free radical polymerization grafting method. This PAAm-g-GaG copolymer hydrogel acts as a drug reservoir and blend films of Guar Gum (GaG) and Polyvinyl Alcohol (PVA) were included as Rate Controlling Membranes (RCM) in the system. The PAAm-g-GaG copolymer was characterized by FTIR, neutralization equivalent values, thermogravimetric analysis and elemental analysis. Results: On the basis of results obtained, it is implicit that the drug permeation decreased with an increase in the concentration of glutaraldehyde and RCM thickness; while drug permeation rate was increased with increasing applied electric current strength from 2 to 8 mA. A two fold increase in flux values was observed with the application of DC electric current. An increase in drug permeation was witnessed under on condition of electric stimulus and permeation was decreased when electric stimulus was "off". The skin histopathology study confirmed the changes in skin structure when electrical stimulus was applied. Conclusion: The electrically-sensitive PAAm-g-GaG copolymer is a useful biomaterial for transdermal drug delivery application.


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