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Pharmacokinetic Study of Solid-Lipid-Nanoparticles of Altretamine Complexed epichlorohydrin-β-cyclodextrin for Enhanced Solubility and Oral Bioavailability

Pharmacokinetic Study of Solid-Lipid-Nanoparticles of Altretamine Complexed epichlorohydrin-β-cyclodextrin for Enhanced Solubility and Oral Bioavailability

Bina Gidwani, Amber Vyas

Int J Biol Macromol. 2017 Aug;101:24-31.

PMID: 28315435

Abstract:

Altretamine is a synthetic drug approved for treatment of ovarian cancer. The only drawback with its formulation is poor aqueous solubility and low oral bioavailability. In the present work an attempt has been made to prepare inclusion complex of altretamine with epichlorohydrin beta cyclodextrin. The complexes were prepared by kneading, co-evaporation and freeze-drying method and were confirmed by FTIR, XRD, DSC, drug content and dissolution study. Kneaded complex possess maximum solubilizing efficiency of 82.63 in 25mM Epi-β-CD solution. SLNs of pure altretamine and ALT complexed with Epi-β-CD were prepared by modified emulsification-ultrasonication method. The particle size and zeta potential was found to be 151.5nm and -21.3mV. The drug release pattern of SLNs was bi-phasic in nature; with an initial burst release followed by sustained drug release. Pharmacokinetic study showed that the average Cmax was found to be 0.94μg/ml, which was 2.47 times higher as compared to the pure drug. The AUCt for SLNs was 150minμgh/ml and 54minμgh/ml for pure ALT suspension which proved that the SLNs exhibited greater absorption compared to the pure drug. Thus, smaller particle size, higher entrapment efficiency and enhanced aqueous solubility led to improvement in oral bioavailability of ALT.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP645056	Altretamine		645-05-6	Price

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