Pharmaceutical evaluation of hydroxycamptothecin nanosuspensions with the action of inhibiting P-gp.
- Author:
Xiao-Hui PU
1
;
Jin SUN
;
Yi-Meng QIN
;
Xiao ZHANG
;
Peng ZHANG
;
Zhong-Gui HE
Author Information
1. Pharmaceutical College of Henan University, Kaifeng 475004, China.
- Publication Type:Journal Article
- MeSH:
ATP-Binding Cassette, Sub-Family B, Member 1;
antagonists & inhibitors;
Antineoplastic Agents, Phytogenic;
administration & dosage;
chemistry;
pharmacokinetics;
Biological Availability;
Calorimetry, Differential Scanning;
Camptothecin;
administration & dosage;
analogs & derivatives;
chemistry;
pharmacokinetics;
Cyclosporine;
chemistry;
Drug Carriers;
Drug Compounding;
Microscopy, Electron, Transmission;
Nanoparticles;
Particle Size;
Solubility;
Suspensions;
X-Ray Diffraction
- From:
Acta Pharmaceutica Sinica
2011;46(7):834-838
- CountryChina
- Language:Chinese
-
Abstract:
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.
