Home
Resources
Publications
Receptor-mediated Hepatocyte-Targeted Delivery of Primaquine Phosphate Nanocarboplex Using a Carbohydrate Ligand

Receptor-mediated Hepatocyte-Targeted Delivery of Primaquine Phosphate Nanocarboplex Using a Carbohydrate Ligand

Vishvesh M Joshi, Padma V Devarajan

Drug Deliv Transl Res. 2014 Aug;4(4):353-64.

PMID: 25787067

Abstract:

Primaquine phosphate is a drug of choice for the treatment of malarial relapse. However, poor drug concentration in the hepatocytes and dose-related toxicity pose severe limitations. We report a nanocarboplex of primaquine phosphate by a simple in situ process using dextran sulphate as a carbohydrate polymer and pullulan as an asialoglycoprotein receptor ligand. Our aim was to preferentially enhance accumulation of the nanocarboplex in the hepatocytes. The in situ pullulan-anchored primaquine nanocarboplex was prepared by simple addition of a solution of dextran sulphate and pullulan with stabilizer to a measured quantity of primaquine phosphate in a vial, followed by shaking to obtain the primaquine phosphate nanocarboplex ready for injection. The nanocarboplex was characterized and evaluated in vivo for pharmacokinetics and biodistribution in the rat model. Specific uptake by hepatocytes in the liver was also quantified. Increase in t ½ with significant uptake in the RES organ was observed. More importantly, anchoring pullulan favored high liver uptake and preferential accumulation in the hepatocytes with a hepatocytes/nonparenchymal cells ratio of 75:25. The in situ primaquine phosphate nanocarboplex anchored with pullulan provides both a significant technological advantage and the desired targeting to the hepatocytes.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP63456	Primaquine phosphate		63-45-6	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: