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Co-delivery of D-(KLAKLAK)2 Peptide and Chlorin e6 using a Liposomal Complex for Synergistic Cancer Therapy

Department of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University, 221 Heukseok dong, Dongjak-gu, Seoul 06974, Korea
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Pharmaceutics 2019, 11(6), 293; https://doi.org/10.3390/pharmaceutics11060293
Received: 4 May 2019 / Revised: 13 June 2019 / Accepted: 19 June 2019 / Published: 21 June 2019
(This article belongs to the Special Issue Advanced Formulation Approaches for Targeted Drug Delivery)
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Abstract

Nanotechnology-based photo-chemo combination therapy has been extensively investigated to improve therapeutic outcomes in anticancer treatment. Specifically, with the help of a singlet oxygen generated by the photosensitizer, the endocytosed nanoparticles are allowed to escape from the endosomal compartment, which is currently an obstacle in nanotechnology-based anticancer therapy. In this study, a liposomal complex system (Lipo (Pep, Ce6)), composed of a chlorin e6-conjugated di-block copolymer (PEG-PLL(-g-Ce6)) and a D-(KLAKLAK)2 peptide loading liposome (Lipo (Pep)), was developed and evaluated for its anticancer activity. Due to the membrane lytic ability of the D-(KLAKLAK)2 peptide and the membrane disruptive effect of the singlet oxygen generated from chlorin e6, Lipo (Pep, Ce6) accelerated the disruption of the endosomal compartment, and exhibited strong synergistic anticancer activity in vitro. The prepared liposomal complex system could potentially maximize the efficacy of the nanotechnology-based photo-chemo combination therapy, and can be regarded as a novel, versatile strategy in advanced tumor therapy. View Full-Text
Keywords: photo-chemo combination therapy; chlorin e6; pro-apoptotic peptide; liposomal complex; endosomal escape photo-chemo combination therapy; chlorin e6; pro-apoptotic peptide; liposomal complex; endosomal escape
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Lim, C.; Kang, J.K.; Won, W.R.; Park, J.Y.; Han, S.M.; Le, T.; Kim, J.C.; Her, J.; Shin, Y.; Oh, K.T. Co-delivery of D-(KLAKLAK)2 Peptide and Chlorin e6 using a Liposomal Complex for Synergistic Cancer Therapy. Pharmaceutics 2019, 11, 293.

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