Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

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• 作者：Mouhamad Khoder^a ; ^{m.khoder@kingston.ac.uk} ; ^{mouhamad.khoder@gmail.com} ; Hamdy Abdelkader^a ; ^b ; Amr ElShaer^a ; Ayman Karam^c ; Mohammad Najlah^d ; Raid G. Alany^a ; ^e
• 关键词：BSA ; bovine serum albumin ; IND ; indometacin ; FD-sol ; freeze dried from solution ; FD-sus ; freeze dried from suspension ; SD-sol ; spray dried from solution ; SD-sus ; spray dried from suspension
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：30 December 2016
• 年：2016
• 卷：515
• 期：1-2
• 页码：740-748
• 全文大小：1546 K
• 卷排序：515

文摘

The aim of this study was to investigate the use of bovine serum albumin (BSA) as a solubility enhancer for indometacin (IND) as a model drug. IND-BSA solid dispersions were prepared by both spray drying and freeze drying techniques using IND:BSA solution (20:1 Molar Ratio (MR)) and IND:BSA suspension (100:1 MR). The solid state of IND in solid dispersions was characterised by SEM, DSC and XRD. The aqueous solubility of IND in the presence of increased amounts of BSA was evaluated. Additionally, IND dissolution and release profiles were evaluated. IND in solid dispersions with BSA showed significantly higher solubility in water than that of the physical mixture of both. Enhancement factors of 24,000 and 100,000 were obtained for the solid dispersion formulated in 20:1 MR and 100:1 MR, respectively. Dissolution studies in-vitro indicated a significant increase in the dissolution rate of IND from solid dispersions compared to that of the free drug, with almost 95% of the drug dissolved in the first 5 min. Furthermore, an immediate release of IND from BSA solid dispersions was shown. The potential use of albumin as solubility enhancer for poorly soluble drugs, particularly, for immediate release volume-limited dosage forms is reported.