Design and Evaluation of Novel Solid Self-Nanodispersion Delivery System for Andrographolide.
Poorly water-soluble drugs offer challenges in developing a formulation product with adequate bioavailability. This study took advantage of the features of nanocrystals and direct compression technologies to develop a novel solid self-nanodispersion delivery system for andrographolide (Andro) in order to increase its dissolution rate for enhancing bioavailability. Andro nanosuspensions (Andro-NS) with a particle size of about 500 nm were prepared by homogenization technology and further converted into dried nanocrystal particles (Andro-NP) via spray-drying. The solid self-nanodispersion delivery system (Andro-SNDS)-loaded Andro-NP was prepared via direct compression technology. The DSC and PXRD results demonstrated that the Andro nanocrystals retained its original crystallinity. The dissolution of the Andro-SNDS formulation was 85.87% in pure water over 30 min, better than those of the coarse Andro and physical mixture of Andro and stabilizer. And the Cmax(299.32 ± 78.54 ng/mL) and AUC0-∞(4440.55 ± 764.13 mg/L · h) of the Andro-SNDS formulation were significantly higher (p < 0.05) than those of the crude Andro (77.52 ± 31.73 ng/mL and 1437.79 ± 354.25 mg/L · h). The AUC of the Andro-SNDS was 3.09 times as high as that of the crude Andro. This study illustrated a novel approach to combine the features of nanocrystals and composite particles used to improve oral bioavailability of poorly soluble drug.
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, 818 Xingwandadao Road, Nanchang, 330004, China.
Junnan
J
Xu
Departments of Pharmacy, 94th Hospital of People's Liberation Army, Nanchang, China.
Yueqin
Y
Ma
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, 818 Xingwandadao Road, Nanchang, 330004, China.
Yuanbiao
Y
Xie
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, 818 Xingwandadao Road, Nanchang, 330004, China.
Yingchong
Y
Chen
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, 818 Xingwandadao Road, Nanchang, 330004, China.
Yang
Y
Liu
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, 818 Xingwandadao Road, Nanchang, 330004, China. feigleYue@outlook.com.
Pengfei
P
Yue
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, 818 Xingwandadao Road, Nanchang, 330004, China.
Ming
M
Yang
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D001682:Biological Availability; D003890:Desiccation; D004224:Diterpenes / Q000008:administration & dosage / Q000493:pharmacokinetics; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D012995:Solubility
D000893:Anti-Inflammatory Agents; D004224:Diterpenes; C030419:andrographolide
andrographolide; bioavailability; nanosuspensions; redispersibility; solid self-nanodispersion delivery system