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        Formulation consideration and skin retention study of microemulsion containing tazarotene for targeted therapy of acne

        Mrunali R. Patel,Rashmin B. Patel,Jolly R. Parikh,Bharat G. Patel 한국약제학회 2016 Journal of Pharmaceutical Investigation Vol.46 No.1

        The objective of this study was to develop and evaluate a novel microemulsion (ME) formulation containing tazarotene for targeted topical therapy of acne. Microemulsions (MEs) were formulated by spontaneous microemulsification method using 12 % Isopropyl myristate, mixed emulsifiers 15 % Labrasol-Cremophor-RH 40 (1:1), 15 % Capmul MCM and 58 % water (w/w) as an external phase. All plain and tazarotene loaded MEs were clear and showed physicochemical parameters for desired topical delivery and stability. The permeation profile of tazarotene through rat skin from selected ME formulation exhibited highest skin uptake. The microscopic observations indicated that the optimized ME had no significant effect on the microscopic structure of the skin and epithelial cells appeared mostly unchanged. The surface epithelium lining and the granular cellular structure of the skin were totally intact. The developed ME may be a potential drug delivery vehicle for targeted topical delivery of tazarotene in the treatment of acne.

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        Microemulsion for nasal delivery of Asenapine maleate in treatment of schizophrenia: formulation considerations

        Mrunali R. Patel,Suresh N. Hirani,Rashmin B. Patel 한국약제학회 2018 Journal of Pharmaceutical Investigation Vol.48 No.3

        The objective of this study was to develop and evaluate the microemulsion (ME) and mucoadhesive microemulsion (MME) for intranasal delivery of Asenapine maleate (APM) for the treatment of schizophrenia. APM loaded ME (AME1 to AME5) and MME (AMME) were prepared by spontaneous microemulsification method and evaluated for drug content, globule size and polydispersity index, % transmittance, zeta potential, pH, viscosity, conductivity, drug content, refractive index, ex vivo diffusion study using sheep nasal mucosa, nasal ciliotoxicity study and Fourier transform infrared spectroscopy study. The AME4 (5 mg/mL of APM) containing 11% Capmul MCM, 38% Smix (Tween80: Propylene glycol (1:1)) and 51% (v/v) water that displayed optical transparency of 99.77%, globule size of 79.50 nm, polydispersity index (PDI) of 0.356 were selected for preparation of MME. The highest diffusion coefficient (P < 0.05) was found for AMME (2.61 × 10−5 ± 0.016 × 10−5 cm2/min) and followed higuchi model. The nasal ciliotoxicity study showed no damage to nasal mucosa and thus the formulation components were considered biocompatible. IR spectra showed no interaction between APM and ME components. Optimized AME and AMME formulations were found to be stable for the period of 6 months. Looking at the results of physicochemical properties and ex vivo studies, it can be concluded that formulated AMME can deliver the APM directly to the brain which has potential of increasing the bioavailability of APM which may alleviate side effects by decreasing the dose and frequency of administration.

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