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BSA-PLGA-Based Core-Shell Nanoparticles as Carrier System for Water-Soluble Drugs

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ABSTRACT

Purpose

Preparation, optimization and in vitro evaluation of core-shell nanoparticles comprising of a hydrophilic core of BSA surrounded by a hydrophobic shell of PLGA for loading water-soluble drugs.

Methods

A double emulsion method was optimized for preparation of BSA-PLGA based core-shell nanoparticles. Proof of concept for core-shell type structure was established by visual techniques like confocal microscopy and TEM. Characterization was done for particle size, encapsulation efficiency, drug loading and in vitro drug release. Cellular uptake was assessed using confocal microscopy, bio-TEM and HPLC assay, and cytotoxic activity was tested by MTT assay in MG-63 osteosarcoma cells.

Results

The optimized core-shell nanoparticles showed a particle size of 243 nm (PDI-0.13) and encapsulation efficiency of 40.5% with a drug loading of 8.5% w/w. In vitro drug release studies showed a sustained release for 12 h. Cellular uptake studies indicated a rapid and efficient uptake within 2 h. TEM studies indicated that the core-shell nanoparticles were localized in cytoplasm region of the cells. Gemcitabine loaded core-shell nanoparticles showed enhanced cytotoxicity against MG-63 cells as compared to marketed formulation of gemcitabine (GEMCITE®).

Conclusion

These results indicate that core-shell nanoparticles can be a good carrier system for delivering hydrophilic drugs like gemcitabine successfully to the cells with enhanced efficacy.

Core-Shell Nanoparticles with a hydrophilic BSA core and hydrophobic PLGA shell for carrier system of hydrophilic drugs

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Abbreviations

BSA:

bovine serum albumin

PLGA:

poly(lactic acid-co-glycolic acid)

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ACKNOWLEDGMENTS AND DISCLOSURES

Financial support from the Department of Biotechnology, India is gratefully acknowledged. Authors are thankful to Department of Science and Technology, India for confocal laser scanning microscope and TEM facilities at NIPER, SAS Nagar. Ranbaxy Science Foundation (RSF), India is duly acknowledged for recognizing this work by awarding Ranbaxy Science Scholar Award-2011 to DC in the field of Pharmaceutical sciences. Support from Dr. Anupama Mittal in conducting cell culture experiments is duly acknowledged.

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Authors and Affiliations

  1. Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S Nagar, Punjab, 160 062, India

    Deepak Chitkara & Neeraj Kumar

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  1. Deepak Chitkara
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  2. Neeraj Kumar
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Corresponding author

Correspondence to Neeraj Kumar.

Electronic Supplementary Material

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Figure S1

DSC thermograms of A) Gemcitabine, B) Blank core-shell nanoparticles, C) Gemcitabine loaded core-shell nanoparticles, D) PLGA and, E) BSA. (JPEG 142 kb)

High resolution (TIFF 348 kb)

Figure S2

XRD diagrams of (A) Gemcitabine, (B) PLGA, (C) BSA, (D) Gemcitabine loaded core-shell nanoparticles and (E) Blank core-shell nanoparticles (JPEG 228 kb)

High resolution (TIFF 320 kb)

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Chitkara, D., Kumar, N. BSA-PLGA-Based Core-Shell Nanoparticles as Carrier System for Water-Soluble Drugs. Pharm Res 30, 2396–2409 (2013). https://doi.org/10.1007/s11095-013-1084-6

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