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Molecules 2016, 21(7), 858; doi:10.3390/molecules21070858

Alendronate-Loaded Modified Drug Delivery Lipid Particles Intended for Improved Oral and Topical Administration

1
Department of Pharmaceutical Technology, Faculty of Pharmacy, Grigore T. Popa University of Medicine and Pharmacy of Iasi, Universitatii Street, 16, Iasi 700115, Romania
2
Petru Poni Institute of Macromolecular Chemistry, Aleea, Grigore Ghica Voda, 41A, Iasi 700487, Romania
3
Department of Natural and Synthetic Polymers, Gheorghe Asachi Technical University of Iasi, Romania, Prof. Dr. Docent Dimitrie Mangeron Avenue, 73, Iasi 700050, Romania
4
Faculty of Mathematics, Alexandru I. Cuza University, 11 Bvd. Carol I, Iasi 700506, Romania
5
Faculty of Mechanical Engineering, Gheorghe Asachi Technical University of Iasi, Romania, Prof. Dr. Docent Dimitrie Mangeron Avenue, 73, Iasi 700050, Romania
6
Faculty of Medicine, Grigore T.Popa University of Medicine and Pharmacy Iasi, 16 Universitatii Street, Iasi 700115, Romania
7
Surgery Department, Sf. Spiridon Hospital, 1 Piata Independentei, Iasi 700111, Romania
8
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Grigore T. Popa University of Medicine and Pharmacy of Iasi, Universitatii Street, 16, Iasi 700115, Romania
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 17 May 2016 / Revised: 24 June 2016 / Accepted: 25 June 2016 / Published: 29 June 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [3112 KB, uploaded 29 June 2016]   |  

Abstract

The present paper focuses on solid lipid particles (SLPs), described in the literature as the most effective lipid drug delivery systems that have been introduced in the last decades, as they actually combine the advantages of polymeric particles, hydrophilic/lipophilic emulsions and liposomes. In the current study, we present our most recent advances in the preparation of alendronate (AL)-loaded SLPs prepared by hot homogenization and ultrasonication using various ratios of a self-emulsifying lipidic mixture of Compritol 888, Gelucire 44/14, and Cremophor A 25. The prepared AL-loaded SLPs were investigated for their physicochemical, morphological and structural characteristics by dynamic light scattering, differential scanning calorimetry, thermogravimetric and powder X-ray diffraction analysis, infrared spectroscopy, optical and scanning electron microscopy. Entrapment efficacy and actual drug content were assessed by a validated HPLC method. In vitro dissolution tests performed in simulated gastro-intestinal fluids and phosphate buffer solution pH 7.4 revealed a prolonged release of AL of 70 h. Additionally, release kinetics analysis showed that both in simulated gastrointestinal fluids and in phosphate buffer solution, AL is released from SLPs based on equal ratios of lipid excipients following zero-order kinetics, which characterizes prolonged-release drug systems. View Full-Text
Keywords: alendronate; Compritol; Gelucire 44/14; Cremophore 25; particles; prolonged release alendronate; Compritol; Gelucire 44/14; Cremophore 25; particles; prolonged release
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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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MDPI and ACS Style

Ochiuz, L.; Grigoras, C.; Popa, M.; Stoleriu, I.; Munteanu, C.; Timofte, D.; Profire, L.; Grigoras, A.G. Alendronate-Loaded Modified Drug Delivery Lipid Particles Intended for Improved Oral and Topical Administration. Molecules 2016, 21, 858.

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