Interactions of primaquine and chloroquine with PEGylated phosphatidylcholine liposomes

Andang Miatmoko, - and Ira Nurjannah, - and Nuril Fadilatul Nehru, - and Noorma Rosita, - and Esti Hendradi, - and Retno Sari, - and Juni Ekowati, - (2021) Interactions of primaquine and chloroquine with PEGylated phosphatidylcholine liposomes. Scientific Reports, 11 (12420). ISSN 2045-2322

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Official URL: https://www.nature.com/articles/s41598-021-91866-0

Abstract

This study aimed to analyze the interaction of primaquine (PQ), chloroquine (CQ), and liposomes to support the design of optimal liposomal delivery for hepatic stage malaria infectious disease. The liposomes were composed of hydrogenated soybean phosphatidylcholine, cholesterol, and distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy[polyethyleneglycol]-2000), prepared by thin film method, then evaluated for physicochemical and spectrospic characteristics. The calcein release was further evaluated to determine the effect of drug co-loading on liposomal membrane integrity. The results showed that loading PQ and CQ into liposomes produced changes in the infrared spectra of the diester phosphate and carbonyl ester located in the polar part of the phospholipid, in addition to the alkyl group (CH2) in the nonpolar portion. Moreover, the thermogram revealed the loss of the endothermic peak of liposomes dually loaded with PQ and CQ at 186.6 °C, which is identical to that of the phospholipid. However, no crystallinity changes were detected through powder X-ray diffraction analysis. Moreover, PQ, with either single or dual loading, produced the higher calcein release profiles from the liposomes than that of CQ. The dual loading of PQ and CQ tends to interact with the polar head group of the phosphatidylcholine bilayer membrane resulted in an increase in water permeability of the liposomes.

Item Type: Article
Subjects: R Medicine
R Medicine > RS Pharmacy and materia medica
R Medicine > RS Pharmacy and materia medica > RS1-441 Pharmacy and materia medica
R Medicine > RS Pharmacy and materia medica > RS200-201 Pharmaceutical dosage forms
Divisions: 05. Fakultas Farmasi > Farmastika
Creators:
CreatorsNIM
Andang Miatmoko, -NIDN0002108503
Ira Nurjannah, --
Nuril Fadilatul Nehru, --
Noorma Rosita, -NIDN0025126506
Esti Hendradi, -NIDN0014115703
Retno Sari, -NIDN0008106303
Juni Ekowati, -NIDN0006026703
Depositing User: Mr M. Fuad Sofyan
Date Deposited: 16 Apr 2023 04:14
Last Modified: 16 Apr 2023 04:14
URI: http://repository.unair.ac.id/id/eprint/123678
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