Maubashera Nawaz, Sofia Hayat, Umer Farooq, Muhammad Adnan Iqbal, Syed Haroon Khalid, Tan Wen Nee, Kooi Yeong Khaw, Rabia Munir and Muhammad Umar Ijaz
{"title":"开发用于烧伤局部治疗的 N-烷基化苯并咪唑立方体水凝胶†。","authors":"Maubashera Nawaz, Sofia Hayat, Umer Farooq, Muhammad Adnan Iqbal, Syed Haroon Khalid, Tan Wen Nee, Kooi Yeong Khaw, Rabia Munir and Muhammad Umar Ijaz","doi":"10.1039/D4RA04816D","DOIUrl":null,"url":null,"abstract":"<p >The current study focuses on assessing the activity of the <em>N</em>-alkylated benzimidazole based cubosomal hydrogel (cubogel) for the topical treatment of burn wounds. The study involves the synthesis of six benzimidazole derivatives (<strong>1–6</strong>) and their characterization by FT-IR and <small><sup>1</sup></small>H and <small><sup>13</sup></small>C NMR spectroscopy. The further study involves the design and formation of nanoparticles known as cubosomes loaded with selected 1-benzyl-1-benzimidazole (API <strong>6</strong>) and the development of a cubogel for the topical treatment of burn wounds. Cubosomes were prepared by the homogenization method, using glyceryl monooleate (GMO) as a lipid polymer and poloxamer 407 (P407) as a surfactant. Cubosomes undergo <em>in vitro</em> characterizations (measurement of particle size, zeta potential, polydispersity index (PDI), % entrapment efficiency, drug release in phosphate buffer saline of pH 6.8, and surface morphology by utilizing TEM (transmission electron microscopy). Formulation D3 (2.5% of GMO, 1% of P407, and 2.5% of PVA) emerged as the optimized formulation, displaying a minimum particle size (PS) of 129.9 ± 1 nm, entrapment efficiency (%EE) of 96.67 ± 0.89%, and a drug release of 86 ± 2.7% at 24 h. Carbopol 940 hydrogel was prepared and incorporated with the optimized formulation to prepare cubogel. This optimized cubogel provided 92.56 ± 0.014% <em>in vitro</em> drug release within 24 h. An <em>in vivo</em> histopathological study was conducted on an animal model (rabbit) to assess the efficacy of cubogel in wound healing and wound contraction. Then cubogel was compared with the commercially available creams Clotrimazole® and Polyfax®. The wound treated with newly developed cubogel has maximum wound contraction (96.70%) as compared to the standard creams. The findings revealed that the newly formulated cubogel was highly effective in treating burns, showing superior performance to commercial products without inducing side effects. Additionally, benzimidazole derivative loaded cubogel caused a sustained release for treating burn wounds without any bacterial infections. The current results further suggested phase 0 clinical trials.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":null,"pages":null},"PeriodicalIF":3.9000,"publicationDate":"2024-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra04816d?page=search","citationCount":"0","resultStr":"{\"title\":\"Development of N-alkylated benzimidazole based cubosome hydrogel for topical treatment of burns†\",\"authors\":\"Maubashera Nawaz, Sofia Hayat, Umer Farooq, Muhammad Adnan Iqbal, Syed Haroon Khalid, Tan Wen Nee, Kooi Yeong Khaw, Rabia Munir and Muhammad Umar Ijaz\",\"doi\":\"10.1039/D4RA04816D\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >The current study focuses on assessing the activity of the <em>N</em>-alkylated benzimidazole based cubosomal hydrogel (cubogel) for the topical treatment of burn wounds. The study involves the synthesis of six benzimidazole derivatives (<strong>1–6</strong>) and their characterization by FT-IR and <small><sup>1</sup></small>H and <small><sup>13</sup></small>C NMR spectroscopy. The further study involves the design and formation of nanoparticles known as cubosomes loaded with selected 1-benzyl-1-benzimidazole (API <strong>6</strong>) and the development of a cubogel for the topical treatment of burn wounds. Cubosomes were prepared by the homogenization method, using glyceryl monooleate (GMO) as a lipid polymer and poloxamer 407 (P407) as a surfactant. Cubosomes undergo <em>in vitro</em> characterizations (measurement of particle size, zeta potential, polydispersity index (PDI), % entrapment efficiency, drug release in phosphate buffer saline of pH 6.8, and surface morphology by utilizing TEM (transmission electron microscopy). Formulation D3 (2.5% of GMO, 1% of P407, and 2.5% of PVA) emerged as the optimized formulation, displaying a minimum particle size (PS) of 129.9 ± 1 nm, entrapment efficiency (%EE) of 96.67 ± 0.89%, and a drug release of 86 ± 2.7% at 24 h. Carbopol 940 hydrogel was prepared and incorporated with the optimized formulation to prepare cubogel. This optimized cubogel provided 92.56 ± 0.014% <em>in vitro</em> drug release within 24 h. An <em>in vivo</em> histopathological study was conducted on an animal model (rabbit) to assess the efficacy of cubogel in wound healing and wound contraction. Then cubogel was compared with the commercially available creams Clotrimazole® and Polyfax®. The wound treated with newly developed cubogel has maximum wound contraction (96.70%) as compared to the standard creams. The findings revealed that the newly formulated cubogel was highly effective in treating burns, showing superior performance to commercial products without inducing side effects. Additionally, benzimidazole derivative loaded cubogel caused a sustained release for treating burn wounds without any bacterial infections. 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Development of N-alkylated benzimidazole based cubosome hydrogel for topical treatment of burns†
The current study focuses on assessing the activity of the N-alkylated benzimidazole based cubosomal hydrogel (cubogel) for the topical treatment of burn wounds. The study involves the synthesis of six benzimidazole derivatives (1–6) and their characterization by FT-IR and 1H and 13C NMR spectroscopy. The further study involves the design and formation of nanoparticles known as cubosomes loaded with selected 1-benzyl-1-benzimidazole (API 6) and the development of a cubogel for the topical treatment of burn wounds. Cubosomes were prepared by the homogenization method, using glyceryl monooleate (GMO) as a lipid polymer and poloxamer 407 (P407) as a surfactant. Cubosomes undergo in vitro characterizations (measurement of particle size, zeta potential, polydispersity index (PDI), % entrapment efficiency, drug release in phosphate buffer saline of pH 6.8, and surface morphology by utilizing TEM (transmission electron microscopy). Formulation D3 (2.5% of GMO, 1% of P407, and 2.5% of PVA) emerged as the optimized formulation, displaying a minimum particle size (PS) of 129.9 ± 1 nm, entrapment efficiency (%EE) of 96.67 ± 0.89%, and a drug release of 86 ± 2.7% at 24 h. Carbopol 940 hydrogel was prepared and incorporated with the optimized formulation to prepare cubogel. This optimized cubogel provided 92.56 ± 0.014% in vitro drug release within 24 h. An in vivo histopathological study was conducted on an animal model (rabbit) to assess the efficacy of cubogel in wound healing and wound contraction. Then cubogel was compared with the commercially available creams Clotrimazole® and Polyfax®. The wound treated with newly developed cubogel has maximum wound contraction (96.70%) as compared to the standard creams. The findings revealed that the newly formulated cubogel was highly effective in treating burns, showing superior performance to commercial products without inducing side effects. Additionally, benzimidazole derivative loaded cubogel caused a sustained release for treating burn wounds without any bacterial infections. The current results further suggested phase 0 clinical trials.
期刊介绍:
An international, peer-reviewed journal covering all of the chemical sciences, including multidisciplinary and emerging areas. RSC Advances is a gold open access journal allowing researchers free access to research articles, and offering an affordable open access publishing option for authors around the world.