[Pharmaceutical evaluation of hydroxycamptothecin nanosuspensions with the action of inhibiting P-gp].
Oral hydroxycamptothecin nanosuspension (HCPT-Nano) with high supersaturated dissolution level, high permeation and well physical stability, was manufactured by microprecipitation-high press homogenization method. Its pharmaceutical properties were investigated, such as size and distribution, zeta potential, particle shape, physical existence condition, supersaturated dissolution level and so on. Particle size was measured by laser diffraction, and the mean diameters before and after lyophilization were 138 +/- 11.72 nm and 175 +/- 12.74 nm, respectively, for HCPT-Nano. Zeta potentials of HCPT-Nano was over -20 mV. The nanoparticles, being observed by transmission electron microscopy (TEM), were claviform or column in shape. DSC and X-ray diffraction revealed that HCPT existed in the form of crystal for HCPT-Nano. And HCPT-Nano could maintain higher supersaturated dissolution level for long time. So it supplied the possibility of improving oral bioavailability of HCPT when combining together admoveatur of P-gp inhibitor, CsA.
Pharmaceutical College of Henan University, Kaifeng 475004, China.
Xiao-Hui
XH
Pu
Jin
J
Sun
Yi-Meng
YM
Qin
Xiao
X
Zhang
Peng
P
Zhang
Zhong-Gui
ZG
He
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002166:Camptothecin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D016572:Cyclosporine / Q000737:chemistry; D004337:Drug Carriers; D004339:Drug Compounding; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D010316:Particle Size; D012995:Solubility; D013535:Suspensions; D014961:X-Ray Diffraction
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D013535:Suspensions; D016572:Cyclosporine; C120029:homocamptothecin; D002166:Camptothecin