alexa 31 P-NMR and Differential Scanning Calorimetry Studies for Determining Vesicle’s Drug Physical State and Fraction in Alendronate Liposomes | OMICS International | Abstract
ISSN: 1948-593X

Journal of Bioanalysis & Biomedicine
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Research Article

31 P-NMR and Differential Scanning Calorimetry Studies for Determining Vesicle’s Drug Physical State and Fraction in Alendronate Liposomes

Eyal Afergan1, Yousef Najajreh2, Dikla Gutman1, Hila Epstein1, Omar Elmalak3 and Gershon Golomb1*

1School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem

2Faculty of Pharmacy, Al-Quds University, Jerusalem

3Biorest Ltd, Yavne, Israel

*Corresponding Author:
Dr. Gershon Golomb
Institute for Drug Research
School of Pharmacy, Faculty of Medicine
The Hebrew University of Jerusalem
12065 Ein Kerem, Jerusalem 91120, Israel
Tel: 972-2-6758658
Fax: 972-2- 6757126
E-mail: [email protected]

Received Date: September 24, 2010; Accepted Date: October 15, 2010; Published Date: October 15, 2010

Citation: Afergan E, Najajreh Y, Gutman D, Epstein H, Elmalak O, et al. (2010) 31P-NMR and Differential Scanning Calorimetry Studies for Determining Vesicle’s Drug Physical State and Fraction in Alendronate Liposomes. J Bioanal Biomed 2:125-131. doi:10.4172/1948-593X.1000035

Copyright: © 2010 Afergan E, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Abstract

Background: A liposomal delivery system requires a complete understanding of the physicochemical characteristics of the drug– liposome system in order to predict their behavior and stability in-vitro and in-vivo .

Objectives: Develop a rapid and simple experimental method to determine the fractions of the drug, alendronate (ALN), encapsulated and as a free form distributed in the liposomal suspension, and the physical state of the encapsulated drug.

Methods: 31 P-NMR measurements utilizing Ga +3 as a shifting reagent in comparison to HPLC determinations, theoretical calculations and differential scanning calorimetry (DSC) studies of various liposomal ALN formulations.

Results: The 31 P-NMR demonstrated that titrating liposomal ALN with increasing amounts of Ga +3 induced a signi fi cant shift in the exterior fraction without changing the interior fraction. Quantitative determination of the encapsulated and non-encapsulated f ractions of ALN has been achieved at Ga +3 concentrations of 3.2-25mM. The DSC study revealed that none of the formulation ingredients is in a solid phase.

Conclusions: 31 P-NMR was found to be sensitive enough to allow accurate differentiation of the distributed fractions of ALN, encapsulated and the non-encapsulated free form. Based on theoretical calculations and DSC analysis it can be concluded that AL N is dissolved in the aqueous core of the liposome.

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