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Encapsulation of exemestane in polycaprolactone nanoparticles: optimization, characterization, and release kinetics.

ABSTRACT: This study was aimed at developing a polymeric drug delivery system for a steroidal aromatase inhibitor, exemestane (exe) intended for sustained targeted delivery of drug through intravenous route. Carboxylated polycaprolactone (cPCL) was synthesized by ring opening polymerization of caprolactone. Exe-loaded cPCL nanoparticles (NPs) were prepared by interfacial deposition of preformed polymer and characterized. A 3-factor, 3-level Box-Behnken design was used to derive a second-order polynomial equation and construct contour and response plots for maximized response of percentage drug entrapment (PDE) with constraints on particle size (PS). The independent variables selected were ratio of exe/cPCL, amount of cPCL, and volume of organic phase. Polymerization of caprolactone to cPCL was confirmed by Fourier transform infrared (FTIR) and gel permeation chromatography. The prepared NPs were evaluated for differential scanning calorimetry (DSC), transmission electron microscopy (TEM), and in vitro release studies. Optimum formulation based on desirability (1.0) exhibited PDE of 83.96 % and PS of 180.5 nm. Check point analysis confirmed the role of the derived polynomial equation and contour plots in predicting the responses. Zeta potential of optimized formulation was -33.8?±?2.1 mV. DSC studies confirmed the absence of any interaction between drug and polymer. TEM image showed non-aggregated and spherical shaped NPs. Drug release from NPs showed sustained release and followed Korsmeyer-Peppas model, indicating Fickian drug release. Thus, preparation of exe-loaded cPCL NPs with high PDE and desired PS suitable for providing passive targeting could be statistically optimized using Box-Behnken design.

SUBMITTER: Kumar A

PROVIDER: S-EPMC4451633 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature

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Encapsulation of exemestane in polycaprolactone nanoparticles: optimization, characterization, and release kinetics.

Kumar Abhinesh A Sawant Krutika K

Cancer nanotechnology 20130425 4-5

This study was aimed at developing a polymeric drug delivery system for a steroidal aromatase inhibitor, exemestane (exe) intended for sustained targeted delivery of drug through intravenous route. Carboxylated polycaprolactone (cPCL) was synthesized by ring opening polymerization of caprolactone. Exe-loaded cPCL nanoparticles (NPs) were prepared by interfacial deposition of preformed polymer and characterized. A 3-factor, 3-level Box-Behnken design was used to derive a second-order polynomial e ...[more]

PMID: 26069501

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Project description:BackgroundBerberine (BBR) broadly found in medicinal plants has a major application in pharmacological therapy as an anticancer drug. Clinical applications of this promising natural drug are limited due to its poor water solubility and low bioavailability.ObjectiveIn this study, for the first time, we synthesized core-shell BBR-loaded PLA nanoparticles (NPBs) by using coaxial electrospray (CES) to solve the poor bioavailability of BBR.MethodsThree-factor (feeding rate, polymeric solution concentration and applied voltage), three-level, Box-Behnken design was used for optimization of the size and particle size distribution of the prepared NPBs.ResultsBased on the results of response surface methodology, the NPBs with the mean size of 265 nm and particle size distribution of 43 nm were synthesized. A TEM image was used to well illustrate the core-shell structure of the NPBs. Encapsulation efficiency and BBR loading capacity for the optimized NPBs were determined at about 81% and 7.5%, respectively. Release of NPBs was examined at pH 7.4 and 5.8. NPBs had a slower release profile than free BBR in both pH values, and the rate of BBR release was more and faster in acidic pH than in physiological one. Effects of the NPBs on the drug release were confirmed by data fitting with six kinetic models. NPBs showed an increased cytotoxic efficacy against HCT116 cells (IC50 = 56 μM), while NIH3T3 cells, non-neoplastic fibroblast cells, (IC50 > 150 μM) were less affected by NPBs. Flow cytometry demonstrated that the cellular uptake of NPBs were higher than BBR at different concentrations.ConclusionsA new approach was developed in this study to prepare NPBs using the CES process for improving the efficiency and controlled BBR release. It is concluded that nano-scaled NPBs prepared by CES can improve toxicity and chemotherapeutic properties of BBR against cancerous cells. We believe that these NPBs can exhibit further potential in cancer drug delivery systems. Graphical abstract.

Dataset Information

Encapsulation of exemestane in polycaprolactone nanoparticles: optimization, characterization, and release kinetics.

Publications

Encapsulation of exemestane in polycaprolactone nanoparticles: optimization, characterization, and release kinetics.

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