Francisco Humberto Xavier-Junior1,2, Nicolas Huang1, Jean-Jacques Vachon1, Vera Lucia Garcia Rehder3, Eryvaldo Sócrates Tabosa do Egito2, Christine Vauthier4. 1. Université Paris-Sud, Institut Galien Paris Sud - UMR CNRS 8612 - Faculté de Pharmacie, 92296, Chatenay-Malabry Cedex, France. 2. Universidade Federal do Rio Grande do Norte, Centro de Ciências da Saúde, Departamento de Farmácia, Laboratório de Sistemas Dispersos (LaSiD), Av. Gal. Gustavo Cordeiro de Farias, S/N, Petrópolis, 59010-180, Natal, RN, Brazil. 3. Universidade Estadual de Campinas (UNICAMP) - Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas. Rua Alexandre Cazelatto, 999, Vila Betel, Paulínia, SP, Brazil. 4. Université Paris-Sud, Institut Galien Paris Sud - UMR CNRS 8612 - Faculté de Pharmacie, 92296, Chatenay-Malabry Cedex, France. christine.vauthier@u-psud.fr.
Abstract
PURPOSE: Aim was to formulate oil-in-water (O/W) microemulsion with a high volume ratio of complex natural oil, i.e. copaiba oil and low surfactant content. The strategy of formulation was based on (i) the selection of surfactants based on predictive calculations of chemical compatibility between their hydrophobic moiety and oil components and (ii) matching the HLB of the surfactants with the required HLB of the oil. METHOD: Solubility parameters of the hydrophobic moiety of the surfactants and of the main components found in the oil were calculated and compared. In turn, required HLB of oils were calculated. Selection of surfactants was achieved matching their solubility parameters with those of oil components. Blends of surfactants were prepared with HLB matching the required HLB of the oils. Oil:water mixtures (15:85 and 25:75) were the titrated with surfactant blends until a microemulsion was formed. RESULTS: Two surfactant blends were identified from the predictive calculation approach. Microemulsions containing up to 19.6% and 13.7% of selected surfactant blends were obtained. CONCLUSION: O/W microemulsions with a high volume fraction of complex natural oil and a reasonable surfactant concentration were formulated. These microemulsions can be proposed as delivery systems for the oral administration of poorly soluble drugs.
PURPOSE: Aim was to formulate oil-in-water (O/W) microemulsion with a high volume ratio of complex natural oil, i.e. copaibaoil and low surfactant content. The strategy of formulation was based on (i) the selection of surfactants based on predictive calculations of chemical compatibility between their hydrophobic moiety and oil components and (ii) matching the HLB of the surfactants with the required HLB of the oil. METHOD: Solubility parameters of the hydrophobic moiety of the surfactants and of the main components found in the oil were calculated and compared. In turn, required HLB of oils were calculated. Selection of surfactants was achieved matching their solubility parameters with those of oil components. Blends of surfactants were prepared with HLB matching the required HLB of the oils. Oil:water mixtures (15:85 and 25:75) were the titrated with surfactant blends until a microemulsion was formed. RESULTS: Two surfactant blends were identified from the predictive calculation approach. Microemulsions containing up to 19.6% and 13.7% of selected surfactant blends were obtained. CONCLUSION: O/W microemulsions with a high volume fraction of complex natural oil and a reasonable surfactant concentration were formulated. These microemulsions can be proposed as delivery systems for the oral administration of poorly soluble drugs.
Authors: T P Formariz; L A Chiavacci; M V Scarpa; A A Silva-Júnior; E S T Egito; C H B Terrugi; C M Franzini; V H V Sarmento; A G Oliveira Journal: Colloids Surf B Biointerfaces Date: 2010-01-14 Impact factor: 5.268
Authors: Bingyue Wang; Tiange Cai; Qian Liu; John Cameron Cole Whitney; Manling Du; Qianqian Ma; Ronghua Zhang; Li Yang; Susan P C Cole; Yu Cai Journal: Int J Mol Med Date: 2018-06-05 Impact factor: 4.101