Characterization of formulation parameters affecting low molecular weight drug release from in situ forming drug delivery systems

Patel, RB; Carlson, AN; Solorio, L; Exner, AA

HERO ID

3539951

Reference Type

Journal Article

Year

2010

Language

English

PMID

20186771

HERO ID 3539951
In Press No
Year 2010
Title Characterization of formulation parameters affecting low molecular weight drug release from in situ forming drug delivery systems
Authors Patel, RB; Carlson, AN; Solorio, L; Exner, AA
Journal Journal of Biomedical Materials Research. Part A
Volume 94
Issue 2
Page Numbers 476-484
Abstract In situ forming implants (ISFI) have shown promise in delivering adjuvant chemotherapy following minimally invasive cancer therapies such as thermal ablation of tumors. Although ISFI systems have been thoroughly investigated for delivery of high molecular weight (Mw) therapeutics, little research has been conducted to optimize their design for delivery of low Mw drugs. This study examined the effect of varying the formulation components on the low Mw drug release profile from a ISFI consisting of poly(D,L-lactide-co-glycolide) (PLGA), fluorescein (model drug), and excipient dissolved in 1-methyl-2-pyrrolidinone (NMP). Effects of varying PLGA Mw, excipient concentration, and drug loading were studied. Additionally, solubility studies were conducted to determine the critical water concentration required for phase inversion. Results demonstrated that PLGA Mw was the most significant factor in modulating low Mw drug release from the ISFI systems. ISFI formulations comprised of a low Mw (16 kDa) PLGA showed a significantly (p < 0.05) lower burst release (after 24 h), 28.2 +/- 0.5%, compared with higher Mw PLGA (60 kDa), 55.1 +/- 3.1%. Critical water concentration studies also demonstrated that formulations with lower Mw PLGA had increased solubility in water and may thus require more time to phase invert and release the drug.
Doi 10.1002/jbm.a.32724
Pmid 20186771
Wosid WOS:000279482600016
Is Certified Translation No
Dupe Override No
Comments Journal: ISSN:
Is Public Yes
Language Text English