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A Polymeric Micellar Carrier for the Solubilization of Biphenyl Dimethyl Dicarboxylate

A Polymeric Micellar Carrier for the Solubilization of Biphenyl Dimethyl Dicarboxylate

Sang-Cheol Chi, Dae-Il Yeom, Sung-Chul Kim, Eun-Seok Park

Arch Pharm Res. 2003 Feb;26(2):173-81.

PMID: 12643597

Abstract:

A polymeric micelle drug delivery system was developed to enhance the solubility of poorly-water soluble drug, biphenyl dimethyl dicarboxylate, DDB. The block copolymers consisting of poly(D,L-lactide) (PLA) as the hydrophobic segment and methoxy poly(ethylene glycol) (mPEG) as the hydrophilic segment were synthesized and characterized by NMR, DSC and MALDI-TOF mass spectroscopy. The size of the polymeric micelles measured by dynamic light scattering showed a narrow monodisperse size distribution with the average diameter less than 50 nm. The MW of mPEG-PLA, 3000 (MW of mPEG, 2 K; MW of PLA, 1 K), and the presence of hydrophilic and hydrophobic segments on the polymeric micelles were confirmed by MALDI-TOF mass spectroscopy and NMR, respectively. Polymeric micelle solutions of DDB were prepared by three different methods, i.e. the matrix method, emulsion method and dialy-sis method. In the matrix method, DDB solubility was reached to 13.29 mg/mL. The mPEG-PLA 2K-1 K micelle system was compared with the poloxamer 407 micelle system for their critical micelle concentration, micelle size, solubilizing capacity, stability in dilution and physical state. DDB loaded-polymeric micelles prepared by the matrix method showed a significantly increased aqueous solubility (>5000 fold over intrinsic solubility) and were found to be superior to the poloxamer 407 micelles as a drug carrier.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP25322683-N	Polyethylene glycol 3000 monodisperse solution		25322-68-3	Price

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