Preparation and in vitro characterization of poly(sebacic acid‐co‐ricinoleic acid)‐based tamoxifen citrate‐loaded microparticles for breast cancer

Abstract

This study was aimed to develop an injectable polymeric drug delivery system for tamoxifen citrate (TC) using poly(sebacic acid-co-ricinoleic acid) [poly(SA-RA) 70 : 30 w/w] as a drug carrier for the treatment of estrogen receptor positive breast cancer. Injectable biodegradable microparticles of TC were produced by solvent displacement technique of microencapsulation and were characterized by surface morphology (scanning electron microscopy), particle size, size distribution, physical and chemical interaction (Fourier transform infrared), nature and physical state of drug [DSC and X-ray diffraction (XRD)], and in vitro release studies. TC loading over different concentrations was analyzed by high performance liquid chromatography (HPLC) technique. Polyanhydride microparticles obtained after lyophilization were nearly spherical in shape with smooth surface and size less than 2.5 lm. TC was dispersed in the form of amorphous state, and TC remains intact and stable during the process of microencapsulation. In vitro drug release studies demonstrated prolonged controlled release of TC with zero-order kinetics. Stability studies revealed that the production process of microparticles itself did not affect the chemical stability of the drug and polymer forming the particle matrix. Significant difference in drug release capacity was observed in microparticles with different drug loadings, and the drug release was more sustained in microparticles prepared with high TC.

An Approach to Enhance Dissolution Rate of Tamoxifen Citrate

“…The effluent was detected at a wavelength of 277 nm. The efficacy of recovery was calculated by dissolving a known quantity of TC in methanol (PBS pH 7.4 (9:1)) and the above procedure was repeated [17]. Each combination was prepared in triplicate to determine the solubility of TC.…”

Paclitaxel loaded poly (DL lactic acid co castor oil) 60:40 with poloxamer‐F68 rod shape cylindrical nanoparticle preparation and in vitro cytotoxicity studies

“…Our previous work supports this circumstance of drug release: We formed tamoxifen citrate as microparticles, and only 90% of the drug was released after 90 hours. During 35 days of dissolution in implants, only 70% of tamoxifen citrate was released using poly (sebacic acid‐co‐ricinoleic acid, 70:30) . Our investigations propose that PTX is released from the nanoparticle as a function of water penetration into the polymer lattice and drug release from the polymer.…”

“…During 35 days of dissolution in implants, only 70% of tamoxifen citrate was released using poly (sebacic acid-co-ricinoleic acid, 70:30). 24,[37][38][39] Our investigations propose that PTX is released from the nanoparticle as a function of water penetration into the polymer lattice and drug release from the polymer. The increase in polymer lattice hydrophobicity reduces the water penetration leading to an increase in interactions between the polymer and the drug was concluded.…”

Poly(sebacic anhydride) nanocapsules as carriers: effects of preparation parameters on properties and release of doxorubicin

“…If the solvent evaporates slowly, this leads to larger sizes of the particles (Hiremath et al, 2012). Various solvents such as tetrahydrofuran (Wu et al, 2000), ethanol (Hiremath et al, 2012) and dichloromethane (DCM) (Shelke and Aminabhavi, 2007;Tang et al, 2009;Ulery et al, 2009) have been utilised for the preparation of PSA-based nanoparticles via either nano-precipitation or emulsion-evaporation methods. Among them, DCM is the most commonly used solvent in the manufacturing of anhydridebased nanoparticles (Pfeifer et al, 2007).…”