Nandhini Sundaresan, Ilango Kaliappan
Divison of Pharmacognosy and Phytochemistry, Interdisciplinary Institute of Indian System of Medicine (IIISM), SRM Institute of Science and Technology, Kattankulathur-603 203, Chengalpattu (Dt), Tamil Nadu, India.
Department of Pharmaceutical Chemistry, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur-603 203, Chengalpattu (Dt), Tamil Nadu, India.
Res Pharm Sci. 2020 Dec 30;16(1):103-117. doi: 10.4103/1735-5362.305193. eCollection 2021 Feb.
Vasicine is a potential bronchodilator and can be used for the effective management of asthma and bronchitis. It has low absorption in the gastrointestinal tract due to its poor solubility thereby low bioavailability. The objective of this research was to develop a novel drug delivery system of vasaka extract to improve its bioavailability by enhancing the solubility and absorption of vasicine.
Vasaka-loaded phytosomes were developed and optimized by thin-layer hydration technique using systematic quality by design approach. Box-Behnken design (3 factorial design) using Design-Expert software was employed to optimize phytosome wherein phosphatidylcholine concentration (X), stirring temperature (X), and stirring time (X) were selected as independent variables. Yield (%), particle size (nm), and entrapment efficiency (%) were evaluated as responses. The optimized phytosome was characterized by studying the surface morphology such as FE-SEM and TEM analysis, thermal characteristics by thermal gravimetric analysis and spectral and diffraction studies by FTIR and XRD analysis and studying the dissolution behaviour of phytosome by release study.
FINDINGS/RESULTS: The percentage yield, particle size, and entrapment efficiency values of the phytosomes were found in the range of 30.03-97.03%, 231.0-701.4 nm, and 20.02-95.88% w/w, respectively. The optimized phytosome showed the zeta potential of -23.2 mV exhibited good stability and SEM and TEM analysis revealed the spherical shape and smooth particles with the uniform particle size distribution of phytosomes. The comparative drug release study of vasaka extract and phytosome revealed the sustained release characteristics of phytosome which reached 68.80% at 8 h compared to vasaka extract reached a maximum of 45.08% at 4 h.
The results highlighted the importance of optimization of formulation development using quality by design strategy to achieve consistent quality of pharmaceutical products.
鸭嘴花碱是一种潜在的支气管扩张剂，可用于有效治疗哮喘和支气管炎。由于其溶解性差，在胃肠道中的吸收较低，因此生物利用度低。本研究的目的是开发一种新型的鸭嘴花提取物药物递送系统，通过提高鸭嘴花碱的溶解度和吸收来提高其生物利用度。
采用系统的质量源于设计方法，通过薄层水化技术制备并优化了载鸭嘴花碱的植物脂质体。使用Design-Expert软件的Box-Behnken设计（3因素设计）来优化植物脂质体，其中选择磷脂酰胆碱浓度（X1）、搅拌温度（X2）和搅拌时间（X3）作为自变量。将产率（%）、粒径（nm）和包封率（%）作为响应指标进行评估。通过研究表面形态（如场发射扫描电子显微镜和透射电子显微镜分析）、热重分析的热特性、傅里叶变换红外光谱和X射线衍射分析的光谱和衍射研究以及通过释放研究来研究植物脂质体的溶解行为，对优化后的植物脂质体进行表征。
植物脂质体的产率、粒径和包封率分别在30.03 - 97.03%、231.0 - 701.4 nm和20.02 - 95.88% w/w范围内。优化后的植物脂质体的ζ电位为-23.2 mV，表现出良好的稳定性，扫描电子显微镜和透射电子显微镜分析显示其呈球形，颗粒光滑，粒径分布均匀。鸭嘴花提取物与植物脂质体的对比药物释放研究表明，植物脂质体具有缓释特性，在8小时时达到68.80%，而鸭嘴花提取物在4小时时最高达到45.08%。
结果强调了使用质量源于设计策略优化制剂开发以实现药品质量一致性的重要性。
