title: Huperzine A-phospholipid complex-loaded biodegradable thermosensitive polymer gel for controlled drug release.
abstract: The huperzine A-phospholipid complex loaded biodegradable thermosensitive PLGA-PEG-PLGA polymer gel was studied as injectable implant system for controlled release of huperzine-A (HA). First, HA molecules were successfully incorporated into the soybean phosphatidylcholine (SP) molecules to form the huperzine-A-soybean phosphatidylcholine complexes (HA-SPC), which was proved by FT-IR, DSC, XRD, solubility study, TEM, etc. The results indicated that hydrogen bonds and electrostatic interaction between HA and SP molecules play an important role in the formation of HA-SPC. Secondly, the HA-SPC was loaded into biodegradable PLGA-PEG-PLGA thermosensitive gel as injectable implant material to control the release of HA. The in vitro and in vivo drug release behaviors of the prepared products were studied. The in vitro release studies demonstrated that the HA-SPC-loaded gel significantly reduced the initial burst of drug release and extended the release period to about 2 weeks. The in vivo pharmacokinetics study of HA-SPC-loaded gel in rabbits showed that plasma concentration of HA (2.54-0.15ng/mL) was detected for nearly 2 weeks from delivery systems upon single subcutaneous injection. What's more, the in vitro release pattern correlated well with the in vivo pharmacokinetics profile. The present study indicates that HA-SPC loaded PLGA-PEG-PLGA thermal gel may be an attractive candidate vehicle for controlled HA release.
authors.affiliation: School of Pharmaceutical Science and Center for Pharmaceutical Research & Drug Delivery Systems, Shandong University, Jinan, Shandong Province 250012, PR China.
authors.forename: Xiaoqing
authors.initials: X
authors.lastname: Cai
authors.forename: Yuxia
authors.initials: Y
authors.lastname: Luan
authors.forename: Yue
authors.initials: Y
authors.lastname: Jiang
authors.forename: Aixin
authors.initials: A
authors.lastname: Song
authors.forename: Wei
authors.initials: W
authors.lastname: Shao
authors.forename: Zhonghao
authors.initials: Z
authors.lastname: Li
authors.forename: Zhongxi
authors.initials: Z
authors.lastname: Zhao
mesh_terms: D000470:Alkaloids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D004343:Drug Implants; D005782:Gels; D007279:Injections, Subcutaneous; D018696:Neuroprotective Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D010713:Phosphatidylcholines / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D011098:Polyglactin 910 / Q000737:chemistry*; D011817:Rabbits; D012717:Sesquiterpenes / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D012995:Solubility; D013025:Glycine max / Q000737:chemistry; D055672:Static Electricity; D013696:Temperature; D013997:Time Factors
chemical_list: D000470:Alkaloids; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004343:Drug Implants; D005782:Gels; D018696:Neuroprotective Agents; D010713:Phosphatidylcholines; D012717:Sesquiterpenes; C528571:poly(lactic-co-glycolic acid)-polyethylene glycol-poly(lactic-co-glycolic acid); C050426:huperzine A; D011098:Polyglactin 910; D011092:Polyethylene Glycols