Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Av. do Café s/n, Ribeirão Preto, SP, 14040-903, Brazil.
Department of Pharmaceutics, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, 220005, Nigeria.
AAPS PharmSciTech. 2020 May 18;21(5):143. doi: 10.1208/s12249-020-01668-2.
This work aims to improve the functionality of Rosmarinus officinalis L. (rosemary) polyphenols by encapsulation in an optimized proliposome formulation. A 2 Box-Wilson central composite design (CCD) was employed to determine lone and interaction effects of composition variables on moisture content (X); water activity (A); concentration and retention of rosemary polyphenols-rosmarinic acid (ROA), carnosol (CAR), and carnosic acid (CNA); and recovery of spray-dried proliposomes (SDP). Processing conditions which generate proliposomes with optimum physicochemical properties were determined by multi-response analysis (desirability approach). Antioxidant and antifungal activities were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) sequestering and minimum inhibitory concentration (MIC)/minimum fungicidal concentration (MFC) assays, respectively. SDP exhibited high polyphenol retention, ranging from 62.0 to 100.0% w/w, showing dependence on composition variables and polyphenol lipophilicity. SDP recovery ranged from 20.1 to 45.8%, with X and A of 1.7 ± 0.14-2.5 ± 0.23% w/w and 0.30 ± 0.004-0.47 ± 0.003, respectively, evidencing product with good chemical and microbiological stability. Optimum liposomal composition was determined, namely, lipid concentration (4.26% w/w), lyophilized extract (LE) concentration (4.48% w/w), and drying aid:(lipid+extract) ratio (7.55% w/w) on wet basis. Relative errors between experimental and predicted values for SDP properties showed concurrence for all responses except CAR retention, being 22% lower. SDP showed high antioxidant activity with IC of 9.2 ± 0.2 μg/mL, superior to results obtained for LE (10.8 μg/mL) and butylated hydroxytoluene (BHT), a synthetic antioxidant (12.5 μg/mL). MIC and MFC against Candida albicans (ATCC1023) were 312.5 μg/mL and 1250 μg/mL, respectively, a moderate antimicrobial activity for phytochemical-based products. SDP is shown as a veritable tool to encapsulate hydrophilic and lipophilic rosemary polyphenols generating a product with optimal physicochemical and biological properties.
本工作旨在通过优化前体脂质体配方,提高迷迭香(Rosmarinus officinalis L.)多酚的功能。采用 2 盒-威尔逊中心组合设计(CCD)来确定组成变量对水分含量(X)、水分活度(A)、迷迭香多酚-迷迭香酸(ROA)、鼠尾草酸(CAR)和鼠尾草酚酸(CNA)的浓度和保留率以及喷雾干燥前体脂质体(SDP)回收率的单因素和交互作用的影响。通过多响应分析(理想点法)确定产生具有最佳物理化学性质的前体脂质体的加工条件。通过 1,1-二苯基-2-苦基肼(DPPH)清除和最小抑菌浓度(MIC)/最小杀菌浓度(MFC)测定法分别评估抗氧化和抗真菌活性。SDP 表现出较高的多酚保留率,范围为 62.0%至 100.0%(w/w),表明对组成变量和多酚亲脂性的依赖性。SDP 回收率范围为 20.1%至 45.8%,X 和 A 分别为 1.7±0.14-2.5±0.23%(w/w)和 0.30±0.004-0.47±0.003,表明产品具有良好的化学和微生物稳定性。确定了最佳的脂质体组成,即:脂质浓度(4.26%(w/w))、冻干提取物(LE)浓度(4.48%(w/w))和干燥助剂:(脂质+提取物)比(7.55%(w/w))在湿基上。除 CAR 保留率外,SDP 性质的实验值和预测值之间的相对误差均在所有响应中一致,误差值低 22%。SDP 表现出高抗氧化活性,IC 为 9.2±0.2μg/mL,优于 LE(10.8μg/mL)和丁基化羟基甲苯(BHT)(12.5μg/mL)的结果。对白色念珠菌(ATCC1023)的 MIC 和 MFC 分别为 312.5μg/mL 和 1250μg/mL,这是植物化学产品的中等抗菌活性。SDP 是一种有效的封装亲水性和亲脂性迷迭香多酚的工具,生成具有最佳物理化学和生物学性质的产品。