scholarly journals In vitro skin penetration of clobetasol from lipid nanoparticles: drug extraction and quantitation in different skin layers

2012 ◽  
Vol 48 (4) ◽  
pp. 811-817 ◽  
Author(s):  
Luís Antônio Dantas Silva ◽  
Stephânia Fleury Taveira ◽  
Eliana Martins Lima ◽  
Ricardo Neves Marreto
Keyword(s):  
Stratum Corneum ◽  
Topical Therapy ◽  
Entrapment Efficiency ◽  
Skin Penetration ◽  
Drug Accumulation ◽  
Uniform Size ◽  
Liquid Chromatographic Method ◽  
Systemic Side Effects ◽  
Liquid Chromatographic

Clobetasol propionate (CP) is a potent topical corticosteroid that causes several cutaneous and systemic side effects. In the present work, CP was encapsulated in nanostructured lipid carriers (NLCs) to increase drug retention in the outer skin layers and improve the safety of topical therapy. NLCs were prepared using a microemulsion technique with a mixture of lecithin, taurodeoxycholate, stearic acid, and oleic acid. In vitro penetration studies were performed in a modified Franz-type diffusion cell, and porcine ears were used as a model of human skin. A simple and sensitive liquid chromatographic method was developed and validated for clobetasol determination in different skin layers. NLCs presented uniform size distribution, high zeta potentialand entrapment efficiency values (> 98%). The analytical procedure was validated according to FDA guidelines. Clobetasol recoveries from skin samples were higher than 85%, with no interference of skin components and NLC ingredients. In experiments, after 6 h, a higher drug accumulation in the stratum corneum arising from NLCs compared to aqueous CP solution was observed. Thus, the NLCs demonstrated high potential for targeting CP to the skin and ensuring drug accumulation in the stratum corneum.

scholarly journals Topical Delivery of Apremilast Loaded Nanostructured Lipid Carrier Based Hydrogel for Psoriasis Therapy

2021 ◽  
pp. 7-20
Author(s):  
S. M. Sindhoor ◽  
Marina Koland
Keyword(s):  
Electron Microscopy ◽  
Transmission Electron Microscopy ◽  
Extended Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Transmission Electron ◽  
Psoriasis Therapy ◽  
Systemic Side Effects

Background: Apremilast (APR) is an orally administered selective phosphodiesterase 4 inhibitor approved to treat plaque psoriasis and psoriatic arthritis and is available as an oral tablet formulation. However, its systemic side effects limit its application. The low solubility and permeability of apremilast make it difficult to administer it through the skin. Hence an attempt is made to incorporate apremilast into a suitable nanocarrier to facilitate its topical delivery. Aims: To formulate and characterize Apremilast loaded nanostructured lipid carriers for the management of psoriasis to reduce the systemic side effects. Methodology: Apremilast loaded Nanostructured Lipid carriers (NLC) were prepared by melt emulsification accompanied by probe sonication. The formulation was prepared using GMS, Sefsol 218, Tween 80 and Transcutol P as Solid Lipid, Liquid lipid, Surfactant and Penetration Enhancer. The NLC was incorporated into carbapol 934 dispersion to convert it into a gel. The NLC formulation was evaluated for size, Polydispersity Index, Zeta Potential, Entrapment efficiency,  Transmission Electron Microscopy. After that, the NLC gel was examined for Spreadability, Extrudabilty, Viscosity, In vitro drug release, Ex vivo permeation, Skin deposition and In vivo studies. Results: The formulated Apremilast loaded showed particle size of less than 200 nm (i.e.170.32nm) with a narrow PDI of 0.267. Entrapment efficiency revealed that 89.26±01.22% of the drug was entrapped. Transmission electron microscopy images confirmed the spherical nature of the nanocarrier. The extended-release pattern of the formulated NLC for 24h was observed in the in vitro release studies and followed the Higuchi model(R2=0.9966). Ex vivo permeability showed a 6.14 fold increase in permeability and 74.05±0.25% deposition of apremilast loaded NLC gel compared to apremilast gel. The formulation was stable for three months without significant changes. In vivo skin studies showed that the prepared NLC did not have any skin irritation potential. The antipsoriatic activity demonstrated by the Apremilast loaded NLC gel in the imiquimod induced psoriasis model in mice was comparable to the standard treatment. Conclusion: Apremilast loaded NLC demonstrated enhanced permeation, improved skin retention and extended-release compared to conventional gel. The developed formulation can be an alternative for psoriasis therapy after clinical trials in the future.

scholarly journals FORMULATION AND EVALUATION OF ELASTIC LIPOSOMES OF DECITABINE PREPARED BY ROTARY EVAPORATION METHOD

2019 ◽  
Author(s):  
Nwobodo Ndubuisi Nwobodo ◽  
Adamude Fatima Amin ◽  
Dingwoke Emeka John ◽  
Abraham Ubhenin
Keyword(s):  
Drug Release ◽  
Dna Methyltransferase ◽  
Entrapment Efficiency ◽  
Skin Penetration ◽  
Topical Administration ◽  
Systemic Circulation ◽  
Stability Study ◽  
Evaporation Method ◽  
Rotary Evaporation

Decitabine is a cytidine deoxynucleoside analog, which acts by inhibiting DNA methyltransferase, and is used for the treatment of acute myeloid leukemia. Decitabine has a short half-life (25 minutes), and is sensitive to harsh conditions. Elastic liposomes are an effective tool that can be used to overcome this disadvantage. Elastic liposomes also known as transfersomes are modified lipid carriers that enable drug to reach deeper skin layers and/or the systemic circulation. These vesicular formulations are several orders of magnitudes, more deformable than the standard liposomes and thus well suited for skin penetration. The objective of present study is to develop and evaluate the elastic liposomes of Decitabine so as to provide the sustained release and improve its bioavailability. Elastic liposomes were prepared by rotary evaporation method using Span 80 and Span 60 as a surfactants. The prepared Elastic liposomes were evaluated for entrapment efficiency, vesicle size, in vitro drug release. The drug release profiles from different elastic liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. Based on different parameters formulations of batch ELS1 was found to be the best formulations. Stability study was performed on the selected formulation ELS1. Study concludes that Decitabine can also be formulated in the liposomal carrier which finds its best way for the topical administration.

scholarly journals Hydrogel composite containing azelaic acid and tea tree essential oil as a therapeutic strategy for Propionibacterium and testosterone-induced acne

2021 ◽  
Author(s):  
Alpna Bisht ◽  
Chetna Hemrajani ◽  
Charul Rathore ◽  
Tania Dhiman ◽  
Rajan Rolta ◽  
...  
Keyword(s):  
Azelaic Acid ◽  
Ternary Phase Diagram ◽  
Acne Vulgaris ◽  
Topical Therapy ◽  
Wistar Rat ◽  
Bacterial Strains ◽  
Uniform Size ◽  
Tea Tree ◽  
Hydrogel Composite

AbstractAzelaic acid (AzA) is a USFDA bioactive prescribed against acne vulgaris. It possesses delivery challenges like poor aqueous solubility, low skin-penetrability, and dose-dependent side effects, which could be overcome by its synergistic combination with tea tree oil (TTO) as a microemulsion (ME)-based hydrogel composite. AzA-TTO ME was prepared to employ pseudo-ternary phase diagram construction. The best AzA-TTO ME was of uniform size (polydispersity index < 0.7), nano-range (~357.4 ± 2% nm), transmittance (> 90%), and negative zeta potential (−1.42 ± 0.25% mV) values. ME hydrogel composite with optimum rheological and textural attributes showed better permeation, retention, and skin-compliant characteristics, vis-a-vis marketed formulation (Aziderm™) when evaluated in Wistar rat skin. In vitro antibacterial efficacy in bacterial strains, i.e., Staphylococcus aureus, Propionibacterium acne, and Staphylococcus epidermidis, was evaluated employing agar well plate diffusion and broth dilution assay. ME hydrogel has shown an increase in zone of inhibition by two folds and a decrease in minimum inhibitory concentration (MIC) by eightfold against P. acnes vis-a-vis AzA. Finally, ME hydrogel composite exhibited a better reduction in the papule density (93.75 ± 1.64%) in comparison to Aziderm™ 72.69 ± 4.67%) on acne as developed in rats by inducing testosterone. Thus, the developed AzA-TTO ME hydrogel composite promises an efficacious and comparatively safer drug delivery system for the topical therapy of acne vulgaris. Graphical abstract

scholarly journals Stratum corneum lipid liposomes for investigating skin penetration enhancer effects

RSC Advances ◽  
2018 ◽  
Vol 8 (48) ◽  
pp. 27464-27469 ◽  
Author(s):  
Mónika Bakonyi ◽  
Attila Gácsi ◽  
Szilvia Berkó ◽  
Anita Kovács ◽  
Erzsébet Csányi
Keyword(s):  
Stratum Corneum ◽  
Skin Penetration ◽  
Penetration Enhancer ◽  
Stratum Corneum Lipid ◽  
Stratum Corneum Lipid Liposomes ◽  
Lipid Liposomes

The aim of this work was to investigate the applicability of stratum corneum lipid liposomes as in vitro skin models for studying skin penetration enhancer effect of Kolliphor RH40 and Transcutol.

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