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Article

Iontosomes: Electroresponsive Liposomes for Topical Iontophoretic Delivery of Chemotherapeutics to the Buccal Mucosa

by 1,2,†, 1,2,‡, 1,2,§ and 1,2,*
1
School of Pharmaceutical Sciences, University of Geneva, CMU-1 Rue Michel Servet, 1211 Geneva, Switzerland
2
Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva, CMU-1 Rue Michel Servet, 1211 Geneva, Switzerland
*
Author to whom correspondence should be addressed.
Present address: Axio Biosolutions Private Limited Plot 18, Gujarat Pharma Techno Park, Sari-Matoda, TA: Sanand, Ahmedabad, Gujarat, India.
Present address: Weber Shandwick Switzerland, 13 Cours de Rive, 1204 Geneva, Switzerland.
§
Present address: School of Pharmacy, Nantong University, 19 Qixiu Road, Nantong 226001, China.
Pharmaceutics 2021, 13(1), 88; https://doi.org/10.3390/pharmaceutics13010088
Received: 16 December 2020 / Revised: 3 January 2021 / Accepted: 5 January 2021 / Published: 11 January 2021
(This article belongs to the Special Issue New Formulations for Cancer Therapy)
The targeted local delivery of anticancer therapeutics offers an alternative to systemic chemotherapy for oral cancers not amenable to surgical excision. However, epithelial barrier function can pose a challenge to their passive topical delivery. The charged, deformable liposomes—“iontosomes”—described here are able to overcome the buccal mucosal barrier via a combination of the electrical potential gradient imposed by iontophoresis and their shape-deforming characteristics. Two chemotherapeutic agents with very different physicochemical properties, cisplatin (CDDP) and docetaxel (DTX), were co-encapsulated in cationic iontosomes comprising 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) and Lipoid-S75. The entrapment of CDDP was improved by formulating it in anionic reverse micelles of dipalmitoyl-sn-glycero-3-phospho-rac-glycerol sodium (DPPG) prior to loading in the iontosomes. Cryo-TEM imaging clearly demonstrated the iontosomes’ electroresponsive shape-deformable properties. The in vitro transport study using porcine mucosa indicated that iontosomes did not enter the mucosa without an external driving force. However, anodal iontophoresis resulted in significant amounts of co-encapsulated CDDP and DTX being deposited in the buccal mucosa; e.g., after current application for 10 min, the deposition of CDDP and DTX was 13.54 ± 1.78 and 10.75 ± 1.75 μg/cm2 cf. 0.20 ± 0.07 and 0.19 ± 0.09 μg/cm2 for the passive controls—i.e., 67.7- and 56.6-fold increases—without any noticeable increase in their transmucosal permeation. Confocal microscopy confirmed that the iontosomes penetrated the mucosa through the intercellular spaces and that the penetration depth could be controlled by varying the duration of current application. Overall, the results suggest that the combination of topical iontophoresis with a suitable nanocarrier system can be used to deliver multiple “physicochemically incompatible” chemotherapeutics selectively to oral cancers while decreasing the extent of systemic absorption and the associated risk of side effects. View Full-Text
Keywords: iontophoresis; deformable liposomes; nanocarrier; oral cancer; drug delivery; buccal mucosa iontophoresis; deformable liposomes; nanocarrier; oral cancer; drug delivery; buccal mucosa
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MDPI and ACS Style

Sonaje, K.; Tyagi, V.; Chen, Y.; Kalia, Y.N. Iontosomes: Electroresponsive Liposomes for Topical Iontophoretic Delivery of Chemotherapeutics to the Buccal Mucosa. Pharmaceutics 2021, 13, 88. https://doi.org/10.3390/pharmaceutics13010088

AMA Style

Sonaje K, Tyagi V, Chen Y, Kalia YN. Iontosomes: Electroresponsive Liposomes for Topical Iontophoretic Delivery of Chemotherapeutics to the Buccal Mucosa. Pharmaceutics. 2021; 13(1):88. https://doi.org/10.3390/pharmaceutics13010088

Chicago/Turabian Style

Sonaje, Kiran, Vasundhara Tyagi, Yong Chen, and Yogeshvar N. Kalia. 2021. "Iontosomes: Electroresponsive Liposomes for Topical Iontophoretic Delivery of Chemotherapeutics to the Buccal Mucosa" Pharmaceutics 13, no. 1: 88. https://doi.org/10.3390/pharmaceutics13010088

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