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Organelle targeting: third level of drug targeting

Authors Sakhrani NM, Padh H

Received 22 March 2013

Accepted for publication 9 May 2013

Published 17 July 2013 Volume 2013:7 Pages 585—599

DOI https://doi.org/10.2147/DDDT.S45614

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 4


Niraj M Sakhrani, Harish Padh

Department of Cell and Molecular Biology, BV Patel Pharmaceutical Education and Research Development (PERD) Centre, Gujarat, India


Abstract: Drug discovery and drug delivery are two main aspects for treatment of a variety of disorders. However, the real bottleneck associated with systemic drug administration is the lack of target-specific affinity toward a pathological site, resulting in systemic toxicity and innumerable other side effects as well as higher dosage requirement for efficacy. An attractive strategy to increase the therapeutic index of a drug is to specifically deliver the therapeutic molecule in its active form, not only into target tissue, nor even to target cells, but more importantly, into the targeted organelle, ie, to its intracellular therapeutic active site. This would ensure improved efficacy and minimize toxicity. Cancer chemotherapy today faces the major challenge of delivering chemotherapeutic drugs exclusively to tumor cells, while sparing normal proliferating cells. Nanoparticles play a crucial role by acting as a vehicle for delivery of drugs to target sites inside tumor cells. In this review, we spotlight active and passive targeting, followed by discussion of the importance of targeting to specific cell organelles and the potential role of cell-penetrating peptides. Finally, the discussion will address the strategies for drug/DNA targeting to lysosomes, mitochondria, nuclei and Golgi/endoplasmic reticulum.

Keywords: intracellular drug delivery, cancer chemotherapy, therapeutic index, cell penetrating peptides

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