Paclitaxel-loaded star-shaped copolymer nanoparticles for enhanced malignant melanoma chemotherapy against multidrug resistance

Abstract

Malignant melanoma (MM) is the most dangerous type of skin cancer with annually increasing incidence and death rates. However, chemotherapy for MM is restricted by low topical drug concentration and multidrug resistance. In order to surmount the limitation and to enhance the therapeutic effect on MM, a new nanoformulation of paclitaxel (PTX)-loaded cholic acid (CA)-functionalized star-shaped poly(lactide-co-glycolide) (PLGA)-D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) nanoparticles (NPs) (shortly PTX-loaded CA-PLGA-TPGS NPs) was fabricated by a modified method of nanoprecipitation. The particle size, zeta potential, morphology, drug release profile, drug encapsulation efficiency, and loading content of PTX-loaded NPs were detected. As shown by confocal laser scanning, NPs loaded with coumarin-6 were internalized by human melanoma cell line A875. The cellular uptake efficiency of CA-PLGA-TPGS NPs was higher than those of PLGA NPs and PLGA-TPGS NPs. The antitumor effects of PTX-loaded NPs were evaluated by the MTT assay in vitro and by a xenograft tumor model in vivo, demonstrating that star-shaped PTX-loaded CA-PLGA-TPGS NPs were significantly superior to commercial PTX formulation Taxol®. Such drug delivery nanocarriers are potentially applicable to the improvement of clinical MM therapy.

Chemodrug delivery using integrin-targeted PLGA-Chitosan nanoparticle for lung cancer therapy

“…2B ]. The drug loading efficiency of our nanoparticle seems reasonable and is consistent with range of drug loading found in literature, from 1% wt/wt 42 to 10.46% wt/wt 43 or higher, that have shown successful therapeutic efficiency.…”

Green synthesis of methoxy-poly(ethylene glycol)-block-poly(l-lactide-co-glycolide) copolymer using zinc proline as a biocompatible initiator for irinotecan delivery to colon cancer in vivo

“…6,7 PLGA copolymers and poly (ethylene glycol) methyl ether-block-poly (lactic-co-glycolic acid) (mPEG-PLGA) copolymers constitute an important class of biologically relevant copolymers. 8,9 They have the propensity to self-assemble into micelles when dispersed in an aqueous medium, depending on composition, making them ideal drug delivery carriers to solubilise hydrophobic drugs. 10,11 In polymer synthesis, stannous octoate is used worldwide as an inexpensive commercial catalyst.…”

Diclofenac-Derived Hybrids for Treatment of Actinic Keratosis and Squamous Cell Carcinoma

“…In particular, Vit-E TPGS was chosen in virtue of its multivalued features as excellent solubilizer and bioavailability enhancer of hybrophobic molecules, as well as to act as selective antitumor agent inducing apoptosis in cancer cells and not healthy ones. Moreover its ability to inhibit the activity of P glycoprotein makes it an important excipient to overcome multidrug resistance that represents an impediment to the success of anticancer therapy [36,37,38]. Nanomicellar formulations containing hybrid 1 were characterized from the physico-chemical point of view.…”