Abstract

Polycaprolactone fumarate (PCLF) is a biocompatible and biodegradable polyester which has been evaluated for tissue engineering. Hydrophobic PCLF nanoparticles (NPs) may be uptaken by reticule endotelial system rich organs and useful for treatment of related tumors. NPs of three PCLFs were produced through nanoprecipitation method. Crosslinked (CR) NPs were prepared using Benzyl peroxide (BPO) and N-vinyl pyrrolidone (NVP) under heating. Doxorubicin HCl (Dox) loaded NPs of PCLF530, 1250 and 2000 showed size of 149, 238 and 274 nm, respectively and zeta potential of about -40 mV, while their drug loadings (DL%) were 2.1, 6.0 and 6.8%, respectively. Dox was released from the NPs in 2 to 4 days in phosphate buffer saline, pH 7.4 at 37°C. Crosslinking of NPs could be completed at BPO/PCLF of 0.01 and NVP/PCLF of 0.1 at 40°C with no change in NP size. PCLF530 NPs possessed a higher CR% than two other NPs. The CR% was reduced in formulations without NVP and with NVP/PCLF of 0.8. Electron microscopic images revealed spherical (CR and not CR) NPs and core-shell structure. PCLF1250 NPs showed both more DL% and smaller size in relation to NPs of PCLF530 and 2000, respectively with a prolonged drug release profile and can be useful as a passive targeted drug delivery system. PCLF NPs could be CR (64.3%) through chemical crosslinking and consequently higher DL% (11.6%), longer drug release (6 days) and smaller size (188 nm) than not CR NPs.

Key words: Crosslinked PCLF NPs, doxorubicin HCl, nanoparticles.

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Abbreviation

PCL, Poly caprolactone; PCLF, poly caprolactone fumarate; NP,nanoparticle; DW, deionized water; PBS, phosphate buffered saline; Dox, doxorubicin HCl; CR, crosslinked; PVA, polyvinyl alcohol; BPO, benzoyl peroxide; DMT, dimethyl toluidine; NVP, N-vinyl pyrrolidone; MC, methylene chloride; THF, tetra hydro furan;DL, drug loading; EE, drug entrapment efficiency; Mw, molecular weight; Tm, melting temperature; PDI, polydispersity index; SD, standard deviation; RES, reticuloendotelial system; SEM, scanning electron microscopy.