Preparation and evaluation of poly-butylcyanoacrylate nanoparticles for oral delivery of thymopentin.
Thymopentin (Tp5) was loaded in poly-butylcyanoacrylate (PBCA) nanoparticles (NP) in order to enhance the oral bioavailability of Tp5. PBCA-Tp5-NP was prepared by nanoprecipitation methods. Dialyzing membrane method was employed to examine the in vitro release of PBCA-Tp5-NP in PBS, and Tp5 samples in the release medium were detected by HPLC. The cell proliferation test ((3)H-thymidine) was conducted to verify the PBCA-Tp5-NP bioactivity in vitro. The pharmacodynamical studies were performed on preimmunoinhibited rats and in flow cytometer. The size and the entrapment efficiency of PBCA-Tp5-NP were 178 +/- 39 nm and 92.21 +/- 1.08%, respectively. In vitro release data show that less than 60% Tp5 was released from lyophilized PBCA-Tp5-NP while 80% Tp5 was released from the colloidal PBCA-Tp5-NPs in 48 h. The proliferation test showed that PBCA-Tp5-NP had the similar effect as Tp5. The in vivo data showed that oral PBCA-Tp5-NPs had similar function as what intravenous Tp5 did. The oral bioavailability of Tp5 could be enhanced by PBCA nanoparticles. PBCA-Tp5-NP had the property of sustained-release and the efficacy of Tp5 was not changed after formulation.
He
Weiling
W
University of Wyoming School of Pharmacy, Laramie, Wyoming 82071, USA.
Jiang
Xuehua
X
Zhang
Zhi-Rong
ZR
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D011232:Chemical Precipitation; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D004659:Enbucrilate / Q000737:chemistry*; D005240:Feasibility Studies; D005260:Female; D005434:Flow Cytometry; D007155:Immunologic Factors / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D008807:Mice, Inbred BALB C; D008956:Models, Chemical; D053758:Nanoparticles; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013499:Surface Properties; D013601:T-Lymphocytes / Q000187:drug effects; D013678:Technology, Pharmaceutical / Q000379:methods; D016305:Thymopentin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D007155:Immunologic Factors; D004659:Enbucrilate; D016305:Thymopentin