Combined formulation of doxorubicin-Arg-Gly-Asp (RGD) and modified PEGylated PLGAencapsulated nanocarrier improves anti-tumor activity

---

Stanley Moffatt, Richard Cristiano and Rose Boyle

Regent University College of Science and Technology, Ghana
University of Texas MD Anderson Cancer Center, USA
University of Hull, UK

: J Nanomater Mol Nanotechnol

Abstract

---

The over-expression of integrin receptors on some malignant cancer cells provides a distinct marker for targeted chemo-therapeutical or diagnostic contrast agent deliveries. Typically, the Arg-Gly-Asp (RGD) peptide, which has high affinity to αvβ3 integrin, has been applied in experimental studies to deliver drugs, gene or imaging agents to the desired targeted sites. In this newly generated formulation, Doxorubicin (Dox) was conjugated to Poly (lactic-co-glycolic acid) (PLGA), and formulated via solvent-diffusion techniques into nanoparticles. The surface of the nanoparticles was subsequently linked with Poly (ethylene glycol) (PEG) and Arg-Gly-Asp (RGD) peptide to achieve both passive and active targeting moieties. The nanoparticles were then tested against several malignant tumor cell lines. The conjugation increased loading efficiency of Dox to PLGA nanoparticles (the encapsulation efficiency was over 85%) and alleviated the drug burst release effect substantially. The drug was released from the polymeric matrix in a sustained release manner over a period of 12 days. The resultant nanoparticles were spherically uniform and well-dispersed. The nanoparticle targeting ability was further proven through strong affinity to various integrin-expressing cancer cells, and much less affinity to the low integrin expression cancer cells. The nanoparticles also showed high efficacy in inducing apoptosis in specific malignant cancer cells. Taken together, these multifunctional nanoparticles hold potential to treat malignant integrin-expressing cancers.

Biography

---

Stanley Saamoah Moffatt is a Distinguished Scholar of Biomedical Science and Nanoengineeringand currently serving as the the Dean of the School of Informatics and Engineering. Before joining Regent-Ghana in 2009, he was a senior researcher at the University of Texas and Assistant Professor at Florida Southeastern University in the United States, where he applied the principles of nanotechnology - engineering at a molecular level - to the design of a new class of nanotechnology - based therapeutics. His research interests include the development and application of shaped polymeric and fabricated nanomaterials for various biomaterials applications, including drug delivery and targeting, research of which incorporates several leading technology platforms including transcriptomics, proteomics, and bioinformatics. He is an astute and prolific researcher whose current research in Biomedical and Genetic Engineering hinges on the formulation and development of active macromolecular biological entities, particularly, nano-encapsulated polymeric particles for tumor delivery. He led a team in the United States in designing and developing a polymer-based therapeutics model involving a novel peptide linkage system for the tumor-specific molecule, CD13, which was published in several peer-reviewed international nanotechnology journals. He has made numerous presentations at various international meetings in the UK, USA and Asia in this interesting and dynamic area of research.