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Effect of different polysorbates on development of self-microemulsifying drug delivery systems using medium chain lipids.
Drug Dev Ind Pharm. 2018 Feb; 44(2):215-223.DD

Abstract

The primary objective of this study was to develop lipid-based self-microemulsifying drug delivery systems (SMEDDS) without using any organic cosolvents that would spontaneously form microemulsions upon dilution with water. Cosolvents were avoided to prevent possible precipitation of drug upon dilution and other stability issues. Different polysorbates, namely, Tween 20, Tween 40, Tween 60, and Tween 80, were used as surfactants, and Captex 355 EP/NF (glycerol tricaprylate/caprate) or its 1:1 mixture with Capmul MCM NF (glycerol monocaprylocaprate) were used as lipids. Captex 355-Tween-water ternary phase diagrams showed that oil-in-water microemulsions were formed only when the surfactant content was high (80-90%) and the lipid content low (10-20%). Thus, mixtures of Tweens with Captex 355 alone were not suitable to prepare SMEDDS with substantial lipid contents. However, when Captex 355 was replaced with the 1:1 mixture of Captex 355 and Capmul MCM, clear isotropic microemulsion regions in phase diagrams with sizes in the increasing order of Tween 20 < Tween 40 < Tween 60 < Tween 80 were obtained. Tween 80 had the most profound effect among all surfactants as microemulsions were formed with lipid to surfactant ratios as high as 7:3, which may be attributed to the presence of double bond in its side chain that increased the curvature of surfactant layer. Thus, lipid-surfactant mixtures containing 1:1 mixture of medium chain triglyceride (Captex 355) and monoglyceride (Capmul MCM) and as low as 30% Tween 80 were identified as organic cosolvent-free systems for the preparation of SMEDDS. Formulations with a model drug, probucol, dispersed spontaneously and rapidly upon dilution with water to form microemulsions without any drug precipitation.

Authors+Show Affiliations

a Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences , St. John's University , Queens , NY , USA.a Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences , St. John's University , Queens , NY , USA. b Celgene Corporation , Summit (West) , NJ , USA.a Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences , St. John's University , Queens , NY , USA.a Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences , St. John's University , Queens , NY , USA. c Abon Pharmaceuticals LLC , Northvale , NJ , USA.d ABITEC Corporation , Columbus , OH , USA.a Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences , St. John's University , Queens , NY , USA.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29057677

Citation

Shah, Ankita, et al. "Effect of Different Polysorbates On Development of Self-microemulsifying Drug Delivery Systems Using Medium Chain Lipids." Drug Development and Industrial Pharmacy, vol. 44, no. 2, 2018, pp. 215-223.
Shah A, Thool P, Sorathiya K, et al. Effect of different polysorbates on development of self-microemulsifying drug delivery systems using medium chain lipids. Drug Dev Ind Pharm. 2018;44(2):215-223.
Shah, A., Thool, P., Sorathiya, K., Prajapati, H., Dalrymple, D., & Serajuddin, A. T. M. (2018). Effect of different polysorbates on development of self-microemulsifying drug delivery systems using medium chain lipids. Drug Development and Industrial Pharmacy, 44(2), 215-223. https://doi.org/10.1080/03639045.2017.1386202
Shah A, et al. Effect of Different Polysorbates On Development of Self-microemulsifying Drug Delivery Systems Using Medium Chain Lipids. Drug Dev Ind Pharm. 2018;44(2):215-223. PubMed PMID: 29057677.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of different polysorbates on development of self-microemulsifying drug delivery systems using medium chain lipids. AU - Shah,Ankita, AU - Thool,Prajwal, AU - Sorathiya,Komal, AU - Prajapati,Hetal, AU - Dalrymple,Damon, AU - Serajuddin,Abu T M, Y1 - 2017/10/23/ PY - 2017/10/24/pubmed PY - 2018/2/6/medline PY - 2017/10/24/entrez KW - Lipid-based drug delivery KW - Tweens® KW - drug dispersion KW - monoglyceride KW - phase diagram KW - polysorbates KW - self-microemulsifying drug delivery systems (SMEDDS) KW - triglyceride SP - 215 EP - 223 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 44 IS - 2 N2 - The primary objective of this study was to develop lipid-based self-microemulsifying drug delivery systems (SMEDDS) without using any organic cosolvents that would spontaneously form microemulsions upon dilution with water. Cosolvents were avoided to prevent possible precipitation of drug upon dilution and other stability issues. Different polysorbates, namely, Tween 20, Tween 40, Tween 60, and Tween 80, were used as surfactants, and Captex 355 EP/NF (glycerol tricaprylate/caprate) or its 1:1 mixture with Capmul MCM NF (glycerol monocaprylocaprate) were used as lipids. Captex 355-Tween-water ternary phase diagrams showed that oil-in-water microemulsions were formed only when the surfactant content was high (80-90%) and the lipid content low (10-20%). Thus, mixtures of Tweens with Captex 355 alone were not suitable to prepare SMEDDS with substantial lipid contents. However, when Captex 355 was replaced with the 1:1 mixture of Captex 355 and Capmul MCM, clear isotropic microemulsion regions in phase diagrams with sizes in the increasing order of Tween 20 < Tween 40 < Tween 60 < Tween 80 were obtained. Tween 80 had the most profound effect among all surfactants as microemulsions were formed with lipid to surfactant ratios as high as 7:3, which may be attributed to the presence of double bond in its side chain that increased the curvature of surfactant layer. Thus, lipid-surfactant mixtures containing 1:1 mixture of medium chain triglyceride (Captex 355) and monoglyceride (Capmul MCM) and as low as 30% Tween 80 were identified as organic cosolvent-free systems for the preparation of SMEDDS. Formulations with a model drug, probucol, dispersed spontaneously and rapidly upon dilution with water to form microemulsions without any drug precipitation. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/29057677/Effect_of_different_polysorbates_on_development_of_self_microemulsifying_drug_delivery_systems_using_medium_chain_lipids_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639045.2017.1386202 DB - PRIME DP - Unbound Medicine ER -