ABSTRACT

AIM: To develop a carrier system for a drug molecule which can show better activity on
breast cancer cells (MCF-7).
Method: The identification and characterization of Centchroman was as per given in
reference standard. Physical appearance and the melting point of the drug sample under
investigation was found silmilarly with I.P.2007. The UV absorption maxima of
Centchroman was obtained at 279 nm.
The drug purity was identified by FT-IR scan was in the accordance with the standard
sample of the drug reported in reference standard. The drug purity was also confirmed by
NMR and Mass spectroscopy and the characteristic peaks obtained were compared with
standard spectra of pue drug reported in reference standard. The solubility of Centchroman
was determined in aqueous and organic solvents.
The estimation of Centchroman was done with HPLC method. The calibration curves
of Centchroman was prepared in the mobile phase consist of 0.04% Tetramethyl Ammonium
Hydroxide (TMAH) buffer and ACN in ratio of 15:85(v/v).
Optimization of formulation was done using polymer PCl and stabilizing agents PF68,
PF127 and Span 80 as surfactant. The particle size were found to be larger with Span80,
PF68 and polydispersity was found to be higher therefore further trials were done and the
optimized formulation was choosen.with stabilizing agent PF127 different formulations were
made.
Result: The optimized nanoparticulate formulation CPNPs8 was prepared using solvent
emulsifaication-evaporation method at various ratios of PCl, PF127 and drug. These drug
loaded PCl nanoparticles were prepared and checked for their particle size and zeta potential.
Particle size obtained was 152.4 nm, and polydispersity index obtained was 0.165, which
showed uniform distribution of particles in the formulation and the zeta potential +21.8
indicates the formulation was near the stability region. The optimized freeze dried
formulation were studied using DSC and AFM.
The in-vitro release of CPNPs8 confirmed fairly sustained release. It showed initial
burst release with up to 51% drug released in first 8 hours followed by sustained release with
about 63% drug released during 48 hours of study. Initial burst release might be due to
discharge of the Centchroman adsorbed at the surface from the matrix.
From the stability study the size change of formulation at 4oC was smaller as
compared to the size change at 25C. So it could be assumed that the best storage temperature
for the formulated nanoparticles (CPNPs8) will be 4C. The results showed that the
formulation was stable after it had been stored for about 30 days time interval.
Conclusion: In-vitro cytotoxicity studies indicated that PCl nanoparticles with Centchroman
(CPNPs8) have more activity towards breast cancer.