title: Preparation and evaluation of andrographolide-loaded microemulsion.
abstract: Andrographolide has a low aqueous solubility and oral bioavailability, which limits its clinical application. Reform the dosage forms of andrographolide to improve its aqueous solubility and oral bioavailability. The formulation, characterisation, stability, anti-inflammatory effect, pharmacokinetics and oral toxicity of andrographolide-loaded microemulsion, were studied. An formulation of O/W microemulsion consisting of an oil phase of isopropyl myristate, a surfactant phase of Tween 80, a co-surfactant of alcohol, and water was found to be ideal, with mean droplet size of 15.9 nm, a high capacity of solubilisation for andrographolide (8.02 mg mL(-1)). Such an andrographolide-loaded microemulsion is stable by monitoring the time, temperature and gravity-dependent change, and has a much better anti-inflammatory effect and a higher biological availability than andrographolide tablets. Besides, it also shows a very low acute oral toxicity. The andrographolide-loaded microemulsion is a promising dosage form of andrographolide.
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, P.R. China.
authors.forename: Hong
authors.initials: H
authors.lastname: Du
authors.forename: Xuezhi
authors.initials: X
authors.lastname: Yang
authors.forename: Haiyan
authors.initials: H
authors.lastname: Li
authors.forename: Liwei
authors.initials: L
authors.lastname: Han
authors.forename: Xiangri
authors.initials: X
authors.lastname: Li
authors.forename: Xiaoying
authors.initials: X
authors.lastname: Dong
authors.forename: Qingwen
authors.initials: Q
authors.lastname: Zhu
authors.forename: Minglei
authors.initials: M
authors.lastname: Ye
authors.forename: Qianjin
authors.initials: Q
authors.lastname: Feng
authors.forename: Xin
authors.initials: X
authors.lastname: Niu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D004224:Diterpenes / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004655:Emulsions; D008297:Male; D009226:Myristates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D013501:Surface-Active Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004224:Diterpenes; D004655:Emulsions; D009226:Myristates; D011136:Polysorbates; D013501:Surface-Active Agents; C008205:isopropyl myristate; C030419:andrographolide