Palei Narahari Narayan, Mohanta Bibhash Chandra, Rajangam Jayaraman, Guptha Prathap Madeswara
Amity Institute of Pharmacy, Amity University, Lucknow, Uttar Pradesh, India.
Department of Pharmacy, Faculty of Health Science, Central University of South Bihar, Gaya, India.
Turk J Pharm Sci. 2024 Jul 12;21(3):199-210. doi: 10.4274/tjps.galenos.2023.93765.
Olmesartan medoxomil (OLM) is a low bioavailability antihypertensive drug. This study aimed to prepare and optimize an OLM niosomal gel and investigate drug permeation a chicken buccal pouch.
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% ) 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.
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/cm, 0.083 mg/cm × hour, and 041 cm/hour, respectively. Histopathological evaluation revealed that the niosomal gel had better permeability than the OLM gel.
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.
奥美沙坦酯(OLM)是一种生物利用度较低的抗高血压药物。本研究旨在制备并优化OLM脂质体凝胶,并研究其在鸡颊囊中的药物渗透情况。
采用薄膜水化技术制备负载OLM的脂质体。评估脂质体的囊泡大小、zeta电位、包封率和药物累积释放百分比。将脂质体加入到卡波姆974P(1.5%)凝胶中,评估脂质体凝胶的药物渗透性。采用Box-Behnken设计对脂质体凝胶的配方进行优化。通过透射电子显微镜(TEM)和傅里叶变换红外辐射分析对优化后的配方进行进一步表征。
优化后的脂质体制剂的粒径和zeta电位分别为296.4 nm和-38.4 mV。基于TEM分析,发现脂质体呈球形。优化后的脂质体凝胶的渗透率、通量和渗透系数分别为0.507 mg/cm、0.083 mg/cm×小时和0.41 cm/小时。组织病理学评估显示,脂质体凝胶的渗透性优于OLM凝胶。
基于OLM脂质体凝胶的结果,可以得出该制剂有助于提高生物利用度,从而产生更好的治疗效果的结论。