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Merck

Nanomiemgel--a novel drug delivery system for topical application--in vitro and in vivo evaluation.

PloS one (2014-12-30)
Jaganmohan Somagoni, Cedar H A Boakye, Chandraiah Godugu, Apurva R Patel, Henrique Antonio Mendonca Faria, Valtencir Zucolotto, Mandip Singh
RESUMEN

The objective of this study was to formulate and evaluate a unique matrix mixture (nanomiemgel) of nanomicelle and nanoemulsion containing aceclofenac and capsaicin using in vitro and in vivo analyses and to compare it to a marketed formulation (Aceproxyvon). Nanomicelles were prepared using Vitamin E TPGS by solvent evaporation method and nanoemulsion was prepared by high-pressure homogenization method. In vitro drug release and human skin permeation studies were performed and analyzed using HPLC. The efficiency of nanomiemgel as a delivery system was investigated using an imiquimod-induced psoriatic like plaque model developed in C57BL/6 mice. Atomic Force Microscopy images of the samples exhibited a globular morphology with an average diameter of 200, 250 and 220 nm for NMI, NEM and NMG, respectively. Nanomiemgel demonstrated a controlled release drug pattern and induced 2.02 and 1.97-fold more permeation of aceclofenac and capsaicin, respectively than Aceproxyvon through dermatomed human skin. Nanomiemgel also showed 2.94 and 2.09-fold greater Cmax of aceclofenac and capsaicin, respectively than Aceproxyvon in skin microdialysis study in rats. The PASI score, ear thickness and spleen weight of the imiquimod-induced psoriatic-like plaque model were significantly (p<0.05) reduced in NMG treated mice compared to free drug, NEM, NMI & Aceproxyvon. Using a new combination of two different drug delivery systems (NEM+NMI), the absorption of the combined system (NMG) was found to be better than either of the individual drug delivery systems due to the utilization of the maximum possible paths of absorption available for that particular drug.

MATERIALES
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Sigma-Aldrich
Capsaicin, ≥95%, from Capsicum sp.
Sigma-Aldrich
N-Ethylmaleimide, purum p.a., ≥99.0% (HPLC)
Sigma-Aldrich
N-Ethylmaleimide, BioUltra, ≥99.0% (HPLC)
Sigma-Aldrich
Capsaicin, natural
Sigma-Aldrich
N-Ethylmaleimide, crystalline, ≥98% (HPLC)
USP
Capsaicin, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Capsaicin, from Capsicum sp., ≥50% (HPLC)
Sigma-Aldrich
Aceclofenac, ≥98% (HPLC)
Supelco
Capsaicin, analytical standard
Supelco
Capsaicin, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
N-Ethylmaleimide, BioXtra, ≥98% (HPLC)
Capsaicin, European Pharmacopoeia (EP) Reference Standard
Aceclofenac for peak identification, European Pharmacopoeia (EP) Reference Standard