1223 POSTER Enhanced Cellular Delivery of Idarubicin by Surface Modification of Propyl Starch Nanoparticles Employing Pteroic Acid Conjugated Polyvinyl Alcohol

Department of Biopharmaceutics and Pharmaceutical Technology, Campus A4 1, Saarland, University, Saarbrücken, Germany.
International Journal of Pharmaceutics (Impact Factor: 3.65). 08/2011; 420(1):147-55. DOI: 10.1016/j.ijpharm.2011.08.030
Source: PubMed


Enhanced intracellular internalization of the anti-cancer active idarubicin (IDA) was achieved through appropriate surface modification of IDA loaded propyl starch nanoparticles. This was conducted by synthesizing pteroic acid modified polyvinyl alcohol (ptPVA) and employing this stabilizer for formulating the said nanoparticles. Pteroic acid attached at the nanoparticles improved the surface protein adsorption of the nanoparticle, a condition which the nanoparticles would largely experience in vitro and in vivo and hence improve their cellular internalization. Spherical, homogenous IDA nanoparticles (214 ± 5 nm) with surface modified by ptPVA were formulated using the solvent emulsification-diffusion technique. The encapsulation efficiency and drug loading amounted around 85%. In vitro release studies indicated a controlled release of IDA. Safety and efficacy of the nanoparticles was confirmed by suitable cellular cytotoxicity assays. Protein binding studies indicated a higher adsorption of the model protein on nanoparticles formulated with ptPVA as compared to PVA. Cellular uptake studies by confocal laser scanning microscopy revealed a higher cellular uptake of ptPVA stabilized nanoparticles thus confirming the proposed hypothesis of higher protein adsorption being responsible for higher cellular internalization.

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    • "Hydrophobic starch derivatives have therefore been developed to overcome this drawback . Dialdehyde starch (Yu, Xiao, Tong, Chen, & Liu, 2007) and propyl starch (Jain et al., 2011; Santander- Ortega et al., 2010) nanoparticles have been fabricated for encapsulation and delivery of lipophilic pharmaceutical agents. Octenyl Succinic Anhydride (OSA) modified starches have also been used to encapsulate food and flavor ingredients (Qi & Xu, 1999). "
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    • "Apoptosis induction is one of the mechanisms which has attracted researchers' attention for fighting against cancer [1]. Doxorubicin [2], daunorubicin [3], idarubicin [4], bleomycin [5], mitomycin C [6], cisplatin [7], plicamycin [8], and carmustine [9] are of the well-known apoptogenic agents; although in order to serve them in targeted drug delivery system, appropriate drug carriers should be employed. Such carriers are aimed to facilitate drug delivery procedure and avoid problems like bioavailability and normal tissue toxicity. "
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