Abstract
Nanoparticles based on biocompatible methoxy poly(ethylene glycol)-b-poly(D,L-lactide) (mPEG113-b-P(D,L)LAn) copolymers as potential vehicles for the anticancer agent oxaliplatin were prepared by a nanoprecipitation technique. It was demonstrated that an increase in the hydrophobic PLA block length from 62 to 173 monomer units leads to an increase of the size of nanoparticles from 32 to 56 nm. Small-angle X-ray scattering studies confirmed the “core-corona” structure of mPEG113-b-P(D,L)LAn nanoparticles and oxaliplatin loading. It was suggested that hydrophilic oxaliplatin is adsorbed on the core-corona interface of the nanoparticles during the nanoprecipitation process. The oxaliplatin loading content decreased from 3.8 to 1.5% wt./wt. (with initial loading of 5% wt./wt.) with increasing PLA block length. Thus, the highest loading content of the anticancer drug oxaliplatin with its encapsulation efficiency of 76% in mPEG113-b-P(D,L)LAn nanoparticles can be achieved for block copolymer with short hydrophobic block.
Highlights
Published: 24 January 2021In the last decades, great attention has been paid to the development of nanoscale vehicles for drug delivery [1,2,3]
The aim of our study was to elucidate the effect of molecular weight of the hydrophobic P(D,L)LA block on the size, structure, morphology, and drug loading of the mPEG-b-P(D,L)LA nanoparticles
The5 residof 16 ual content of monomer determined by 1 H NMR was less than 1% for all block copolymers
Summary
Published: 24 January 2021In the last decades, great attention has been paid to the development of nanoscale vehicles for drug delivery [1,2,3]. Platinum-based complexes (cisplatin, carboplatin, oxaliplatin, etc.) are widely used chemotherapeutics agents for the treatment of various types of cancer [5,6]. Cisplatin (cis-(eblock)dichloridoplatinum(II)) is the first-generation platinum drug, that has a therapeutic effect against breast cancer, ovarian cancer, lung and head and neck cancer, cervix carcinoma, etc. It produces significant side effects such as ototoxicity, hematological, and emetogenicity [7]. Oxaliplatin ((trans-R,R-cyclohexane-1,2-diamine)oxalatoplatinum(II)) is the third-generation platinum complex that was designed to overcome cellular resistance to cisplatin and carboplatin. Oxaliplatin shows higher solubility and less toxicity than cisplatin.
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