{"title":"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","authors":"Narahari Narayan Palei, Bibhash Chandra Mohanta, Jayaraman Rajangam, Prathap Madeswara Guptha","doi":"10.4274/tjps.galenos.2023.93765","DOIUrl":null,"url":null,"abstract":"<p><strong>Objectives: </strong>Olmesartan medoxomil (OLM) is a low bioavailability antihypertensive drug. This study aimed to prepare and optimize an OLM niosomal gel and investigate drug permeation <i>via</i> a chicken buccal pouch.</p><p><strong>Materials and methods: </strong>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% <i>w/v</i>) 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.</p><p><strong>Results: </strong>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<sup>2</sup>, 0.083 mg/cm<sup>2</sup> × hour, and 041 cm/hour, respectively. Histopathological evaluation revealed that the niosomal gel had better permeability than the OLM gel.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":23378,"journal":{"name":"Turkish Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.8000,"publicationDate":"2024-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Olmesartan Medoxomil-Loaded Niosomal Gel for Buccal Delivery: Formulation, Optimization, and <i>Ex Vivo</i> Studies.\",\"authors\":\"Narahari Narayan Palei, Bibhash Chandra Mohanta, Jayaraman Rajangam, Prathap Madeswara Guptha\",\"doi\":\"10.4274/tjps.galenos.2023.93765\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Objectives: </strong>Olmesartan medoxomil (OLM) is a low bioavailability antihypertensive drug. This study aimed to prepare and optimize an OLM niosomal gel and investigate drug permeation <i>via</i> a chicken buccal pouch.</p><p><strong>Materials and methods: </strong>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% <i>w/v</i>) 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.</p><p><strong>Results: </strong>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<sup>2</sup>, 0.083 mg/cm<sup>2</sup> × hour, and 041 cm/hour, respectively. Histopathological evaluation revealed that the niosomal gel had better permeability than the OLM gel.</p><p><strong>Conclusion: </strong>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.</p>\",\"PeriodicalId\":23378,\"journal\":{\"name\":\"Turkish Journal of Pharmaceutical Sciences\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2024-07-12\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Turkish Journal of Pharmaceutical Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.4274/tjps.galenos.2023.93765\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Turkish Journal of Pharmaceutical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4274/tjps.galenos.2023.93765","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
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.