PolySciTech (
www.polyscitech.com)
provides a wide array of block copolymers including triblock PLGA-PEG-PLGA.
Recently PLGA-PEG-PLGA was utilized to generate a micelle delivery system for
poorly soluble Andrographolide. Read more: Zhang, Jinming, Yingbo Li, Wei Gao,
Michael A. Repka, Yitao Wang, and Meiwan Chen. "Andrographolide-loaded
PLGA-PEG-PLGA micelles to improve its bioavailability and anticancer
efficacy." Expert opinion on drug delivery 0 (2014): 1-14. http://informahealthcare.com/doi/abs/10.1517/17425247.2014.924503
“Abstract: Background: Andrographolide (ADG)
isolated from Andrographis paniculata exhibits anti-inflammatory and anticancer
activities, but high hydrophobicity and poor bioavailability greatly restricts
its clinical application.Objectives: In this study, ADG was encapsulated in a
micelle formulation based on poly (D,L-lactide-co-glycolide)-b-poly (ethylene
glycol)-b-poly (D,L-lactide-co-glycolide) (PLGA-PEG-PLGA) amphiphilic triblock
copolymers, in order to enhance the anticancer efficacy and bioavailability in
vivo. Methods: The physicochemical properties of the ADG-loaded PLGA-PEG-PLGA
micelles were investigated for encapsulation efficiency, particle size, zeta
potential and critical micelle concentration. These micelles were further
evaluated for in vitro cytotoxicity, including proliferation inhibition, cell
cycle arrest and pro-apoptosis effects against human breast cancer MAD-MB-231
cells, cellular uptake and pharmacokinetics study in rat. Results: ADG-loaded
PLGA-PEG-PLGA micelles had a high encapsulation and loading efficiency of about
92 and 8.4% (w/w), respectively, and a stable particle size of 124.3 ± 6.4 nm.
In vitro cytotoxicity testing demonstrated that ADG-loaded PLGA-PEG-PLGA
micelles exhibited higher proliferation inhibition, cell cycle arrest at the
G2/M phase and pro-apoptosis effects in MAD-MB-231 cells, which would be
contributed to higher efficiency of cellular uptake and intracellular
transport. Further, the plasma AUC(0 – ∞) and mean resident time of ADG-loaded
PLGA-PEG-PLGA micelles were increased by 2.7- and 2.5-fold, respectively, when
compared to the raw suspension. Conclusion: All of these investigations suggest
that PLGA-PEG-PLGA micelles may be a potential drug delivery strategy for
improving ADG bioavailability and efficacy in cancer therapy. Keywords andrographolide,
breast cancer MAD-MB-231 cells, micelles, pharmacokinetics, poly
(D,L-lactide-co-glycolide)-b-poly (ethylene glycol)-b-poly
(D,L-lactide-co-glycolide) triblock copolymer”
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