Rosita Noorma, Ambarwati Nadya, Erawati Tristiana, Hariyadi Dewi Melani
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Airlangga, Surabaya, Indonesia.
J Adv Pharm Technol Res. 2022 Jan-Mar;13(1):11-17. doi: 10.4103/japtr.japtr_263_21. Epub 2022 Jan 21.
This study purposes to develop solid lipid microparticles (SLM) inhalation delivery system for respiratory diseases with Quercetin as the active agent. Quercetin has various functions, such as for antioxidant, anti-inflammatory, immunomodulator, and antivirus. SLM is formed from a mixture of lipids and surfactants, namely, Glyceryl Behenate as solid lipid, Poloxamer 188 as the surfactant, and production of SLM using the melt o/w emulsification technique and was dried using freeze dryer. The effect of lipid concentration was studied in this research. Quercetin SLM was characterized by moisture content, Fourier transform infrared, particle size, yield, drug loading, and encapsulation efficiency. The SLM particles produced were spherical in shape and had a smooth surface with sizes of F1, F2, and F3 were 1.79 μm, 1.88 μm, and 1.91 μm, respectively. According to the target particle size of inhalation, Quercetin SLM had good flowability according to Carr's Index (F1 = 12.73% ± 0.38, F2 = 14.28% ± 0.65, F3 = 14.65% ± 0.62), in which the highest drug loading and EE of F3 were 10.94% and 88.48%, respectively. release study showed that in 630 min about 31%-33% Quercetin released indicated sustained release following Higuchi kinetics and quercetin release rate was not affected by the amount of lipid. To sum up, quercetin SLM demonstrates its potential as an inhalation delivery system and it is recommended to study its stability.
本研究旨在开发以槲皮素为活性剂的用于呼吸道疾病的固体脂质微粒(SLM)吸入给药系统。槲皮素具有多种功能,如抗氧化、抗炎、免疫调节和抗病毒等。SLM由脂质和表面活性剂混合物形成,即山嵛酸甘油酯作为固体脂质,泊洛沙姆188作为表面活性剂,采用熔融o/w乳化技术制备SLM,并使用冷冻干燥机进行干燥。本研究考察了脂质浓度的影响。通过水分含量、傅里叶变换红外光谱、粒径、产率、载药量和包封率对槲皮素SLM进行表征。所制备的SLM颗粒呈球形,表面光滑,F1、F2和F3的粒径分别为1.79μm、1.88μm和1.91μm。根据吸入给药的目标粒径,槲皮素SLM根据卡尔指数具有良好的流动性(F1 = 12.73% ± 0.38,F2 = 14.28% ± 0.65,F3 = 14.65% ± 0.62),其中F3的最高载药量和包封率分别为10.94%和88.48%。释放研究表明,在630分钟内约31%-33%的槲皮素释放,表明其符合Higuchi动力学的缓释特性,且槲皮素释放速率不受脂质用量的影响。综上所述,槲皮素SLM显示出作为吸入给药系统的潜力,建议对其稳定性进行研究。