Preparation, Characterization, and Evaluation of Liposomes Containing Oridonin from Rabdosia rubescens

• Published in: Molecules (Basel, Switzerland) Vol. 27; no. 3; p. 860
• Main Authors: Wang, Yinyue, Wang, Mai, Lin, Feier, Zhang, Xinyan, Zhao, Yongming, Guo, Chunyan, Wang, Jin
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 27.01.2022; MDPI
• Subjects: Bioavailability; Biocompatibility; Biological activity; Breast cancer; Cholesterol; Cytotoxicity; Design of experiments; Design optimization; Diterpenes, Kaurane - chemistry; Diterpenes, Kaurane - pharmacokinetics; Diterpenes, Kaurane - pharmacology; Drug delivery; Drug delivery systems; Ethanol; Humans; Isodon - chemistry; Liposomes; MCF-7 Cells; oridonin; Particle Size; Phospholipids; Polydispersity; Prostate; Rabdosia rubescens; Response surface methodology; Soybeans; Tumors; Ultrasonic imaging; ultrasound-assisted extraction; Variables; Water baths; Zeta potential; China; oridonin; ultrasound-assisted extraction; liposomes; Rabdosia rubescens
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules27030860

Due to the remarkable anti-tumor activities of oridonin (Ori), research on has attracted more and more attention in the pharmaceutical field. The purpose of this study was to extract Ori from by ultrasound-assisted extraction (UAE) and prepare Ori liposomes as a novel delivery system to improve the bioavailability and biocompatibility. Response surface methodology (RSM), namely Box-Behnken design (BBD), was applied to optimize extraction conditions, formulation, and preparation process. The results demonstrated that the optimal extraction conditions were an ethanol concentration of 75.9%, an extraction time of 35.7 min, and a solid/liquid ratio of 1:32.6. Under these optimal conditions, the extraction yield of Ori was 4.23 mg/g, which was well matched with the predicted value (4.28 mg/g). The optimal preparation conditions of Ori liposomes by RSM, with an ultrasonic time of 41.1 min, a soybean phospholipids/drug ratio of 9.6 g/g, and a water bath temperature of 53.4 °C, had higher encapsulation efficiency (84.1%). The characterization studies indicated that Ori liposomes had well-dispersible spherical shapes and uniform sizes with a particle size of 137.7 nm, a polydispersity index (PDI) of 0.216, and zeta potential of -24.0 mV. In addition, Ori liposomes presented better activity than free Ori. Therefore, the results indicated that Ori liposomes could enhance the bioactivity of Ori, being proposed as a promising vehicle for drug delivery.