The influence of mPEG-PCL and mPEG-PLGA on encapsulation efficiency and drug-loading of SN-38 NPs

Abstract

The influence of mPEG-PCL and mPEG-PLGA on encapsulation efficiency and drug-loading of nanoparticles was very important. SN-38 NPs were prepared from a series of diblock copolymers: mPEG1000-PLGA2000, mPEG2000-PCLs, mPEG5000-PCLs, mPEG2000-PLGAs, and mPEG5000-PLGAs by the thin filmhydration method. The prepared nanoparticles were characterized by morphology, size, encapsulation efficiency, drug-loading, and in vitro release behavior. This experiment suggested that the encapsulation efficiency and drug-loading of SN-38 NPs were attained the maximum values when the ratio of hydrophilic to hydrophobic block was between 1:2 and 1:3. ARTICLE HISTORY

pH-responsive delivery vehicle based on RGD-modified polydopamine-paclitaxel-loaded poly (3-hydroxybutyrate-co-3-hydroxyvalerate) nanoparticles for targeted therapy in hepatocellular carcinoma

“…The entrapment efficiency (EE) and drug loading efficiency (LE) of RGD-PDA-PHBV-PTX-NPs were determined by HPLC (LC 1200, Agilent Technologies, Santa Clara, CA, USA) methods [30]. In brief, 10 mg of RGD-PDA-PHBV-PTX-NPs were dissolved in 2 mL of methanol under vigorous vortexing.…”

Microfluidic encapsulation of SN-38 in block copolymer nanoparticles: effect of hydrophobic block composition on loading and release properties

“…are typical of SN-38 encapsulation in aliphatic polyester-based PNPs, due to the low solubility of the drug molecules in the associated polymer cores during physical encapsulation. 11 In fact, the only block copolymer SN-38 nanomedicine that has completed phase III trials, NK012, relies on covalent attachment rather than physical encapsulation to entrap the drug within micellar PNPs of SN-38-conjugated poly(glutamic acid)-block-poly(ethylene oxide) (PGA-b-PEO). [4][5][6] However, methods to obtain high SN-38 loading levels via the simpler approach of physical encapsulation by increasing the solubility of the drug within the core-forming block, would certainly be desirable.…”

“…3 Encapsulating SN-38 in a polymer nanoparticle (PNP) takes advantage of the EPR effect to target drug delivery toward tumour tissues. 1,[4][5][6][7][8][9][10][11][12][13] Amphiphilic block copolymers spontaneously form micellar PNPs with a hydrophilic external corona and a hydrophobic internal core. The SN-38 can be contained within the water-dispersible PNPs, which travel to target tissues through the circulatory system.…”

“…Various polymer types have been researched to optimize delivery, including those with hydrophobic blocks comprised of poly(lactic-co-glycolic acid) D r a f t 4 (PLGA), 12 polygluamate (PGlu), [4][5][6] and poly(ε-caprolactone) (PCL). 8,11,13 Poly(ε-caprolactone)b-poly(ethylene oxide) (PCL-b-PEO) is a commonly applied amphiphilic block copolymer in drug delivery investigations, due to the biodegradable and biocompatible nature of its component blocks. 14 Although the hydrolytic degradation of PCL makes it an appropriate in vivo host for a wide variety therapeutic molecules, its semicrystalline nature can strongly influence drug delivery properties.…”

“…15,16,18 In addition, SN-38 generally shows low solubility in aliphatic polyesters including PCL and PLGA. 11 Together these features highlight a need for studies involving systematic variation in block copolymer hydrophobic block composition and crystallinity, in order to gain insights en route to improved materials for SN-38 delivery systems.…”