Microemulsion for nasal delivery of Asenapine maleate in treatment of schizophrenia: formulation considerations
作者： Mrunali R. Patel , Suresh N. Hirani , Rashmin B. Patel
DOI: 10.1007/S40005-017-0318-8
关键词: Bioavailability 、 Mucous membrane of nose 、 Chromatography 、 Fourier transform infrared spectroscopy 、 Dispersity 、 Chemistry 、 Zeta potential 、 Microemulsion 、 Polyvinyl alcohol 、 Nasal administration
摘要: The objective of this study was to develop and evaluate the microemulsion (ME) mucoadhesive (MME) for intranasal delivery Asenapine maleate (APM) treatment schizophrenia. APM loaded ME (AME1 AME5) MME (AMME) were prepared by spontaneous microemulsification method evaluated drug content, globule size polydispersity index, % transmittance, zeta potential, pH, viscosity, conductivity, refractive ex vivo diffusion using sheep nasal mucosa, ciliotoxicity Fourier transform infrared spectroscopy study. AME4 (5 mg/mL APM) containing 11% Capmul MCM, 38% Smix (Tween80: Propylene glycol (1:1)) 51% (v/v) water that displayed optical transparency 99.77%, 79.50 nm, index (PDI) 0.356 selected preparation MME. highest coefficient (P < 0.05) found AMME (2.61 × 10−5 ± 0.016 cm2/min) followed higuchi model. showed no damage mucosa thus formulation components considered biocompatible. IR spectra interaction between components. Optimized AME formulations be stable period 6 months. Looking at results physicochemical properties studies, it can concluded formulated deliver directly brain which has potential increasing bioavailability may alleviate side effects decreasing dose frequency administration.
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