Abstract

Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf.

Background: Different types of lipids can be conjugated with drugs by covalent or non- covalent association to overcome some problems of drug delivery. The aim of this study is to identify and quantify binding sites of phosphatidylcholine in its conjugate with the model drug mefenamic acid (MA-PC) from which pharmacosomes were prepared and evaluated in comparison with conventional liposomes.
Method: Solvent evaporation method was used to prepare MA-PC conjugate and the conjugation sites were confirmed using DSC, P-XRD, 1H-NMR, 13C-NMR, 31P-NMR, FT-IR, and SEM. Physical properties and dissolution study for the drug, conjugate, and the prepared liposomes were studied.
Results: Conjugation was confirmed between the drug and phosphatidylcholine (PC) through mainly hydrogen bond between –COOH group of mefenamic acid (MA) and phosphate polar head of PC in a ratio of 1:1 mainly. The solubility and partition coefficient of MA in its conjugate were significantly higher than pure MA. Pharmacosomal dispersion was prepared using MA-PC conjugate and evaluated in comparison to conventional liposomes prepared with the same lipid ratio, where it showed higher entrapment efficiency (% EE) than conventional liposomes with more rigid morphology. The sequential in-vitro dissolution profile revealed significantly higher dissolution for pharmacosomes than conventional liposomes and much higher than marketed MA suspension.
Conclusion: The phosphate group in PC is the predominant binding site for its conjugation with MA in 1:1 ratio, conjugation improved the drug physical properties in its conjugate and pharmacosomal dispersion in a significant way than the conventionally prepared liposomes in the same ratio.

How to Cite this Article

Pubmed Style Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf. Identification and Quantitation of Phospholipid Binding Sites in Lipid Drug Conjugate Pharmacosomes using Model Drug. SRP. 2020; 11(5): 458-463. doi:10.31838/srp.2020.5.63 Web Style Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf. Identification and Quantitation of Phospholipid Binding Sites in Lipid Drug Conjugate Pharmacosomes using Model Drug. http://www.sysrevpharm.org/?mno=111889 [Access: March 30, 2021]. doi:10.31838/srp.2020.5.63 AMA (American Medical Association) Style Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf. Identification and Quantitation of Phospholipid Binding Sites in Lipid Drug Conjugate Pharmacosomes using Model Drug. SRP. 2020; 11(5): 458-463. doi:10.31838/srp.2020.5.63 Vancouver/ICMJE Style Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf. Identification and Quantitation of Phospholipid Binding Sites in Lipid Drug Conjugate Pharmacosomes using Model Drug. SRP. (2020), [cited March 30, 2021]; 11(5): 458-463. doi:10.31838/srp.2020.5.63 Harvard Style Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf (2020) Identification and Quantitation of Phospholipid Binding Sites in Lipid Drug Conjugate Pharmacosomes using Model Drug. SRP, 11 (5), 458-463. doi:10.31838/srp.2020.5.63 Turabian Style Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf. 2020. Identification and Quantitation of Phospholipid Binding Sites in Lipid Drug Conjugate Pharmacosomes using Model Drug. Systematic Reviews in Pharmacy, 11 (5), 458-463. doi:10.31838/srp.2020.5.63 Chicago Style Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf. "Identification and Quantitation of Phospholipid Binding Sites in Lipid Drug Conjugate Pharmacosomes using Model Drug." Systematic Reviews in Pharmacy 11 (2020), 458-463. doi:10.31838/srp.2020.5.63 MLA (The Modern Language Association) Style Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf. "Identification and Quantitation of Phospholipid Binding Sites in Lipid Drug Conjugate Pharmacosomes using Model Drug." Systematic Reviews in Pharmacy 11.5 (2020), 458-463. Print. doi:10.31838/srp.2020.5.63 APA (American Psychological Association) Style Abdullah Q. Khudhur, Nidhal K. Maraie, Ayad M.R. Raauf (2020) Identification and Quantitation of Phospholipid Binding Sites in Lipid Drug Conjugate Pharmacosomes using Model Drug. Systematic Reviews in Pharmacy, 11 (5), 458-463. doi:10.31838/srp.2020.5.63