奥美沙坦酯-甲氧杂环己酯口腔给药胶:配方、优化和离体研究

IF 1.8 Q3 PHARMACOLOGY & PHARMACY Turkish Journal of Pharmaceutical Sciences Pub Date : 2024-07-12 DOI:10.4274/tjps.galenos.2023.93765
Narahari Narayan Palei, Bibhash Chandra Mohanta, Jayaraman Rajangam, Prathap Madeswara Guptha
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引用次数: 0

摘要

目的:奥美沙坦酯是一种生物利用度低的降压药。本研究旨在制备和优化OLM niosomal凝胶,并研究药物通过鸡颊袋的渗透性。方法:采用膜水化技术制备OLM负载的羊膜。对囊泡大小、ζ电位、包封效率和药物累积释放百分比进行了评估。将niosomes掺入Carbopol 974P(1.5%w/v)凝胶中,并评估niosomes凝胶的药物渗透性。使用Box-Behnken设计优化了niosomal凝胶的配方。使用透射电子显微镜(TEM)和FTIR分析对优化的配方进行了进一步表征。结果:优化后的niobody制剂的粒径和ζ电位分别为296.4nm和-38.4mV。通过透射电镜分析,发现该囊泡呈球形。结果表明,优化后的niobody凝胶的渗透性、通量和渗透系数分别为0.507mg/cm2、0.083mg/cm2×h和041cm/h。组织病理学评估显示,与OLM凝胶相比,羊膜体凝胶具有更好的渗透性。结论:基于OLM羊膜凝胶的结果,可以得出结论,该制剂有利于提高生物利用度,从而产生更好的治疗效果。
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Olmesartan Medoxomil-Loaded Niosomal Gel for Buccal Delivery: Formulation, Optimization, and Ex Vivo Studies.

Objectives: Olmesartan medoxomil (OLM) is a low bioavailability antihypertensive drug. This study aimed to prepare and optimize an OLM niosomal gel and investigate drug permeation via a chicken buccal pouch.

Materials and methods: OLM-loaded niosome were prepared using a film hydration technique. The vesicle size, zeta potential, entrapment efficiency, and percentage cumulative drug release of niosome were evaluated. The niosomes were incorporated into a Carbopol 974P (1.5% w/v) gel, and the drug permeability of the niosomal gel was evaluated. The formulations of the niosomal gel were optimized using the Box-Behnken design. The optimized formulation was further characterized by transmission electron microscopy (TEM) and Fourier transform infrared radiation analysis.

Results: The particle size and zeta potential of the optimized niosomal formulations were 296.4 nm and -38.4 mV, respectively. Based on TEM analysis, the niosomes were found to be spherical in shape. The permeability, flux, and permeability coefficient of the optimized niosomal gel were 0.507 mg/cm2, 0.083 mg/cm2 × hour, and 041 cm/hour, respectively. Histopathological evaluation revealed that the niosomal gel had better permeability than the OLM gel.

Conclusion: Based on the results of the OLM niosomal gel, it can be concluded that the formulation can be beneficial in increasing bioavailability, resulting in better therapeutic efficacy.

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CiteScore
3.60
自引率
5.90%
发文量
79
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