Biocompatible Amphiphilic Pentablock Copolymeric Nanoparticles for Anti-Cancer Drug Delivery

Abstract

A pentablock copolymer of Poly(Lactide-co-Glycolide) and Pluronic F68 was synthesized using ring-opening polymerization and characterized by NMR and FTIR for confirming the structure of the block copolymer. TG-DTA studies showed PLGA:Pluronic ratio to be 4:1. As the PLGA-PEO-PPO-PEO-PLGA Pentablock Copolymer (PPPC) prepared is amphiphilic, its Critical Vesicular Concentration, was measured, which was lower at 37 degrees C than at 25 degrees C, which could provide better stability to the system at physiological temperature. The nanoparticles of PPPC vary in topographyand range from 150 to 500 nm in size, according to the synthesis route used viz Emulsion Solvent Evaporation and simple dialysis. Pentablock copolymer nanoparticles were found to entrap about 84% of hydrophobic drug, docetaxel. Drug release profile of docetaxel showed about 50% release in first 2 hours at pH 4.6 and about 80% docetaxel was released at pH 7.4, at the end of 2 days. The PPPC nanoparticles was found to be biocompatible to L929 cell lines up to 1 mg/ml concentration. Preliminary in vitro cytotoxic effect of docetaxel loaded PPPC nanoparticles against four different cancer cell lines showed 50% inhibitory concentration of 6 nM in A431 (Squamous cell carcinoma), 250 nM in HeLa (Cervical carcinoma), 800 nM in PC3 (Prostate carcinoma) and 1 microM in KB (Epidermoid carcinoma) cells.

Self-assembling surfactant-like peptide A6K as potential delivery system for hydrophobic drugs

“…Despite the success of novel strategies such as soluble derivatives or prodrugs, [1][2][3] the strategy using a delivery system is still a predominant approach, particularly considering its potential to achieve targeted delivery or codelivery of different components. [4][5][6] In recent years, various types of materials have been investigated as delivery systems for hydrophobic drugs, including, but not limited to, liposomes, 7 polymeric nanoparticles, [8][9][10] hydrogels, 11,12 and carbon nanotubes. [13][14][15] Several wellstudied materials have been developed into clinically available formulations, such as Abraxane ® and Doxil ® .…”

Synthesis and Micellar Characterization of CBABC Type PLGA-PEO-PPO-PEO-PLGA Pentablock Copolymers

“…Figure 5 shows the weight change for five kinds of pentablock copolymers up to 500 is no free PLGA chains polymerized independent of F68 polymer chains. 44 The weight percent at the end point of phase I (i.e. 260 o C) were measured as 67.7, 53.9, 45.9, 36.5, and 30.4, which correspond to P1, P2, P3, P4, and P5, respectively.…”

“…Very recently, a similar pentablock copolymer was reported to supply more stable carrier for the anti-cancer drug delivery. 44 However, the synthesis was conducted at high temperature of 160 o C and the amount of independent PLGA units unlinked with F68 was detected as around 11 wt %. 44 Also, the synthesized pentablock copolymer was reported for only one kind of molecular weight (i.e.…”

“…44 However, the synthesis was conducted at high temperature of 160 o C and the amount of independent PLGA units unlinked with F68 was detected as around 11 wt %. 44 Also, the synthesized pentablock copolymer was reported for only one kind of molecular weight (i.e. weight ratio of PLGA:F68 ≈ 4:1) while this manuscript reports different range of PLGA/ F68 up to 2.57.…”

Possible role of nanocarriers in drug delivery against cervical cancer

“…Docetaxel-loaded biocompatible amphiphilic pentablock copolymeric nanoparticles synthesized using poly(lactide-co-glycolide) and pluronic F68 by emulsion solvent evaporation and simple dialysis showed a significant cytotoxicity against cervical cancer cells [60]. A combination therapy consisting of multidrug-incorporated layered double hydroxide nanohybrids has been proved to be an efficient treatment for cervical cancer.…”