Abstract:
The main objectives of this research were to synthesize and evaluated
some novel functionalized polymers to fabricate, formulate and evaluate
in various polymeric matrices of once a day controlled release tablets of
Propionic acid analogs, mainly Ibuprofen, Flurbiprofen and Ketoprofen
and preparation and development of nanoparticles drug delivery systems
to study their release pattern, rate and the involved mechanism in release
process of the drug and to develop and evaluate such sustained release
drug formulations which can be used less frequent and with more patient
compliance. Three new polymers were synthesized including PGA, PGA-
co-caprolactone and PGA-co-pentadecalactone. The polymer backbone
consisting of two ester-linked, non-toxic, biological monomers, glycerol
and polyvinyl adipate, was prepared using a hydrolytic enzyme. A novel
polymeric prodrug was also developed by coupling a model drug,
Ibuprofen, to polyester, poly (glycerol-adipate-co-pentadecalactone), via
ester linkage. Ibuprofen-loaded nanoparticles were also prepared. The
polymers, conjugate and nanoparticles were evaluated and characterized
by GPC, NMR, FT-IR, U.V, and DSC. Among the three polymers, the
particles
of
Ibuprofen
coupled
with
poly
(glycerol-adipate-co-
pentadecalactone) showed a burst release followed thereafter by very
slow release into pH 7.4 phosphate buffer.
Solubility of the drugs was checked by the use of UV. Spectrophotometer
(1601-Shimadzu. Japan) as described by the method of Higuchi and
Connors. In this preformulation study, six solvents were used including
Phosphate buffers of pH 7.4, 7.2 and 6.8, 0.1 N NaoH, 0.1 N HCl solution
and distilled water.
