Topical delivery of clobetasol propionate loaded microemulsion based gel for effective treatment of vitiligo: Ex vivo permeation and skin irritation studies

2013 ◽  
Vol 102 ◽  
pp. 86-94 ◽  
Author(s):  
Hetal K. Patel ◽  
Bhavesh S. Barot ◽  
Punit B. Parejiya ◽  
Pragna K. Shelat ◽  
Arunkumar Shukla
Keyword(s):  
Effective Treatment ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Topical Delivery ◽  
Clobetasol Propionate ◽  
Ex Vivo Permeation ◽  
Microemulsion Based Gel

Development and Evaluation of Particulate Microcarriers of Adapalene as a Topical Delivery System

2019 ◽  
Vol 9 (3) ◽  
pp. 222-233
Author(s):  
Divya D. Jain ◽  
Namita D. Desai
Keyword(s):  
Patient Compliance ◽  
Targeted Delivery ◽  
Ex Vivo ◽  
Acne Vulgaris ◽  
Drug Loading ◽  
Topical Therapy ◽  
Skin Irritation ◽  
Topical Delivery ◽  
Diffusion Method ◽  
Topical Gel

Background: Adapalene is a promising third generation retinoid used in the topical treatment of acne vulgaris. However, the major drawback associated with conventional topical therapy of Adapalene is the ‘retinoid reaction’ which is dose-dependent and characterized by erythema, scaling and burning sensation at the application sites. Microparticulate drug delivery can play a major role in reducing side effects and providing better patient compliance due to targeted delivery. Methods: Adapalene microparticles were prepared using quasi emulsion solvent diffusion method. The effects of formulation variables including polymer ratios, amounts of emulsifier, drug loading and process variables such as stirring time and speed on the physical characteristics of microparticles were investigated. The developed microparticles were characterized by DSC and SEM. Adapalene microparticles were incorporated into Carbopol 971 NF gel for ease of topical delivery. Results: Adapalene microparticulate topical gel showed sustained drug release over 8 hours in in vitro studies. The amount of drug retained in the rat skin during ex vivo studies was higher in the microparticulate topical gel (227.43 ± 0.83 µg/cm2) as compared to the marketed formulation (81.4 ± 1.11 µg/cm2) after 8 hours indicating localized and sustained drug action that can be useful in treating acne vulgaris. The safety of optimized Adapalene gel determined by skin irritation studies performed on Sprague Dawley rats showed no irritation potential. Conclusion: Microparticles can provide promising carrier systems to deliver Adapalene, improving patient compliance due to enhanced skin deposition, localized and sustained action with reduced associated irritant effects.

scholarly journals Design and Optimization of Cationic Nanocapsules for Topical Delivery of Tretinoin: Application of the Box-Behnken Design, In Vitro Evaluation, and Ex Vivo Skin Deposition Study

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Saeed Ebrahimi ◽  
Reza Mahjub ◽  
Rasool Haddadi ◽  
Seyed Yaser Vafaei
Keyword(s):  
Particle Size ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Free Drug ◽  
Acrylic Polymer ◽  
Box Behnken Design

Cationic nanocapsules represent a promising approach for topical delivery purposes. We elaborated on a novel formulation based on the cationic nanocapsules to enhance the pharmacodynamic efficacy, user compliance, and photostability of tretinoin (TTN). To achieve this goal, TTN nanocapsules were prepared by the nanoprecipitation method. In order to statistically optimize formulation variables, a Box-Behnken design, using Design-Expert software, was employed. Three independent variables were evaluated: total weight of the cationic acrylic polymer ( X 1 ), oil volume ( X 2 ), and TTN amount ( X 3 ). The particle size and encapsulation efficiency percent (EE%) were selected as dependent variables. The optimal formulation demonstrated spherical morphology under scanning electron microscopy (SEM), optimum particle size of 116.3 nm, and high EE% of 83.2%. TTN-loaded nanocapsules improved photostability compared to its methanolic solution. The in vitro release study data showed that tretinoin was released in a sustained manner compared to the free drug. The ex vivo skin permeation study demonstrated that greater drug deposition into the epidermal region rather than the deep skin was observed with a gel containing TTN-loaded nanocapsules than that of drug solution, respectively. The skin irritation test revealed that the nanoencapsulation of the drug decreased its irritancy compared to the free drug. These results revealed the promising potential of cationic nanocapsules for topical delivery of tretinoin

scholarly journals Development, Optimization, and Evaluation of Luliconazole Nanoemulgel for the Treatment of Fungal Infection

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Nabil A. Alhakamy ◽  
Shadab Md ◽  
Md Shoaib Alam ◽  
Rasheed A. Shaik ◽  
Javed Ahmad ◽  
...  
Keyword(s):  
Fungal Infections ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Statistical Design ◽  
Entrapment Efficiency ◽  
Application Site ◽  
Ex Vivo Permeation ◽  
Irritation Test ◽  
The Stability ◽  
Skin Irritation Test

The present study aimed to optimize luliconazole nanoemulsion using Box–Behnken statistical design, which was further incorporated into the polymeric gel of Carbopol 934. The formulation was characterized for its size, entrapment efficiency, ex vivo permeation, and mechanism of release. The size of the dispersed globules of the optimized drug-loaded nanoemulsion was found to be 17 ± 3.67 nm with a polydispersity index (PDI) less than 0.5. Although the surface charge was recorded at –9.53 ± 0.251, the stability was maintained by the polymeric matrix that prevented aggregation and coalescence of the dispersed globules. The luliconazole-nanoemulgel (LUL-NEG) was characterized for drug content analysis, viscosity, pH, and refractive index, where the results were found to be 99.06 ± 0.59%, 9.26 ± 0.08 Pa.s, 5.65 ± 0.17, and 1.31 ± 0.08, respectively. The permeation across the rat skin was found to be significantly higher with LUL-NEG when compared with LUL gel. Furthermore, the skin irritation test performed in experimental animals revealed that the blank NEG, as well as the LUL-NEG, did not produce any signs of erythema following 48 h exposure. In addition, the histopathological findings of the experimental skins reported no abnormal signs at the formulation application site. Finally, the NEG formulation was found to create a statistically significant zone of inhibition ( P  < 0.05) when compared to all other test groups. Overall, it could be summarized that the nanoemulgel approach of delivering luliconazole across the skin to treat skin fungal infections could be a promising strategy.

scholarly journals Development and In Vitro/In Vivo Evaluation of pH-Sensitive Polymeric Nanoparticles Loaded Hydrogel for the Management of Psoriasis

Nanomaterials ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 3433
Author(s):  
Muhammad Imran Asad ◽  
Dildar Khan ◽  
Asim ur Rehman ◽  
Abdelhamid Elaissari ◽  
Naveed Ahmed
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Topical Formulation ◽  
Sustained Drug Release ◽  
In Vivo Evaluation ◽  
Ex Vivo Permeation ◽  
Pasi Score

Methotrexate (MTX), the gold standard against psoriasis, poses severe problems when administered systemically viz increased toxicity, poor solubility and adverse reactions. Hence, a topical formulation of MTX for the management of psoriasis can be an effective approach. The present study aimed to develop an MTX based nanoparticle-loaded chitosan hydrogel for evaluating its potential efficacy in an imiquimod-induced psoriatic mice model. MTX-NPs loaded hydrogel was prepared and optimized using the o/w emulsion solvent evaporation method. Particle size, zeta potential, entrapment efficiency, in vitro drug release, ex vivo permeation, skin irritation and deposition studies were performed. Psoriatic Area and Severity Index (PASI) score/histopathological examinations were conducted to check the antipsoriatic potential of MTX-NPs loaded hydrogel using an imiquimod (IMQ)-induced psoriatic model. Optimized MTX-NPs showed a particle size of 256.4 ± 2.17 nm and encapsulation efficiency of 86 ± 0.03%. MTX-NPs loaded hydrogel displayed a 73 ± 1.21% sustained drug release in 48 h. Ex vivo permeation study showed only 19.95 ± 1.04 µg/cm2 of drug permeated though skin in 24 h, while epidermis retained 81.33% of the drug. A significant decrease in PASI score with improvement to normalcy of mice skin was observed. The developed MTX-NPs hydrogel displayed negligible signs of mild hyperkeratosis and parakeratosis, while histopathological studies showed healing signs of mice skin. So, the MTX-NPs loaded hydrogel can be a promising delivery system against psoriasis.

scholarly journals PRONIOSOMAL GEL MEDIATED TRANSDERMAL DELIVERY OF GLIBENCLAMIDE AND ATENOLOL COMBINATION: EXVIVO AND PHARMACODYNAMIC STUDIES

2021 ◽  
pp. 242-248
Author(s):  
P. ANITHA ◽  
S. V. SATYANARAYANA
Keyword(s):  
Transdermal Delivery ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Prediction Method ◽  
Albino Rats ◽  
Box Behnken Design ◽  
Steady State Flux ◽  
Ex Vivo Permeation ◽  
Diabetic Hypertensive Patient ◽  
Wistar Albino Rats

Objective: The objective of the present work was to develop an optimized dosage form for treating comorbidity in combination and evaluate it for its pharmacodynamic performance in male Wistar albino rats. Methods: Transdermal proniosomal gel for Combination of Glibenclamide (GLB) and Atenolol (ATN) was developed and optimized by Box Behnken design. This optimized combinational proniosomal gel (OCPG), which was selected by a point prediction method, was evaluated for its ex vivo, skin irritation studies and pharmacodynamic activities of both drugs in rats in comparison with its oral therapy. Results: The ex-vivo permeation behavior through different skins was studied and the findings were also confirmed by the values of the steady-state flux (Jss). The OCPG observed an increase of more than twice in the cumulative amount of impregnated drugs compared to pure drug films. The study on skin irritation revealed the non-irritability of the developed OCPG applied. OCPG significantly showed sustained hypoglycemic activity in rats (p<0.001), when compared to orally treat animals up to 24 h. Systolic blood pressure (SBP) lowering effect of OCPG was found to be significant (p<0.02), when compared to orally treat rats up to 24 h. However, the reduction was slow and sustained in the case of OPCG where a significant response was observed in the performed studies. Conclusion: Overall, the results show that controlled release GLB and ATN proniosomes offer a useful and promising transdermal delivery system. Henceforth this may be an achievement in treating the diabetic hypertensive patient.

Formulation by Design (FbD) approach to develop pharmaceutically amended Diclofenac Sodium hydrogel as compared to marketed gel

2021 ◽  
Vol 4 (1) ◽  
pp. 3-10
Author(s):  
Anupam Sarma ◽  
◽  
Tapash Chakraborty ◽  
Sheikh Sofiur Rahman ◽  
Abdul Baquee Ahmed ◽  
...  
Keyword(s):  
Propylene Glycol ◽  
Ex Vivo ◽  
Diclofenac Sodium ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Ex Vivo Permeation ◽  
Product Profile ◽  
Permeation Studies ◽  
Carbopol 934P

The aim of the present study was to develop pharmaceutically better performing Diclofenac Sodium hydrogel through FbD approaches as compared to marketed gel. The quality target product profile was set for the critical quality attributes of the gel. The key material variables like Carbopol 934P, propylene glycol and Triethanolamine (TEA) were optimized using design of experiments. A response surface central composite design was used considering viscosity, pH and cumulative percentage permeation of the drug up to 120 min as responses. TEA had a significant effect on the pH at concentrations of 0.3182-3.6818% (w/w). The applicability of the optimized formulations was influenced by both Carbopol 934P (0.6591-2.3409%; w/w) and propylene glycol (PG; 6.591-23.409%; w/w) content due to their ability to alter the formulation viscosity. The optimized formulation, determined mathematically, contained 1.5% (w/w) Carbopol 934P. 2.0% (w/w) TEA and 15% (w/w) PG. The optimized hydrogel and marketed gel were evaluated for viscosity, spreadability, skin irritation, homogeneity and grittiness, texture analysis, in vitro release and ex vivo permeation studies. When these evaluation parameters were compared with a marketed gel in respect of all the evaluating tests, the optimized hydrogel was found to be far better formulation than the marketed one.

Development and Ex-vivo Evaluation of Topiramate Mucoadhesive Nanoparticles for Intranasal Delivery

2020 ◽  
Vol 13 (6) ◽  
pp. 5250-5255
Author(s):  
Ashwin Kumar Tulasi ◽  
Anil Goud Kandhula ◽  
Ravi Krishna Velupula
Keyword(s):  
Particle Size ◽  
Nasal Mucosa ◽  
Intranasal Administration ◽  
Ex Vivo ◽  
Chemical Properties ◽  
Brain Targeting ◽  
Oral Tablet ◽  
Promising Alternative ◽  
Ex Vivo Permeation

Topiramate is a second-generation antiepileptic drug used in partial, generalized seizures as an oral tablet. Oral route of administration is most convenient but shows delayed absorption. Moreover, in emergency cases, parenteral administration is not possible as it requires medical assistance. Hence, the present study was aimed to develop topiramate mucoadhesive nanoparticles for intranasal administration using ionotropic gelation method. The developed nanoparticles were evaluated for physico-chemical properties like particle size, zeta potential, surface morphology, drug content, entrapment efficiency, in vitro drug release, mucoadhesive strength, and ex vivo permeation studies in excised porcine nasal mucosa. Optimized nanoparticle formulation (T9) was composed oil mucoadhesive agent (Chitosan 1% w/w), cross linking polymer (TPP) and topiramate 275mg, 100mg and 4% respectively. It showed particle size of 350nm, high encapsulation efficacy and strong mucoadhesive strength. In vitro drug diffusion of optimized formulation showed 95.12% release of drug after 180min. Ex-vivo permeation of drug across nasal mucosa was   88.05 % after 180min. Nasocilial toxicity studies showed optimized formulation did not damage the nasal mucosa. Thus, the intranasal administration of topiramate using chitosan can be a promising alternative for brain targeting and the treatment of epilepsy.

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