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Development of self-microemulsifying drug delivery system for oral delivery of poorly water-soluble nutraceuticals.
Drug Dev Ind Pharm. 2018 Jun; 44(6):895-901.DD

Abstract

The objective of the study was to develop a self-microemulsifying drug delivery system (SMEDDS), also known as microemulsion preconcentrate, for oral delivery of five poorly water-soluble nutraceuticals or bioactive agents, namely, vitamin A, vitamin K2, coenzyme Q10, quercetin and trans-resveratrol. The SMEDDS contained a 1:1 mixture (w/w) of Capmul MCM NF (a medium chain monoglyceride) and Captex 355 EP/NF (a medium chain triglyceride) as the hydrophobic lipid and Tween 80 (polysorbate 80) as the hydrophilic surfactant. The lipid and surfactant were mixed at 50:50 w/w ratio. All three of the SMEDDS components have GRAS or safe food additive status. The solubility of nutraceuticals was determined in Capmul MCM, Captex 355, Tween 80, and the SMEDDS (microemulsion preconcentrate mixture). The solubility values of vitamin A palmitate, vitamin K2, coenzyme Q10, quercetin, and trans-resveratrol per g of SMEDDS were, respectively, 500, 12, 8, 56, and 87 mg. Appropriate formulations of nutraceuticals were prepared and filled into hard gelatin capsules. They were then subjected to in vitro dispersion testing using 250 mL of 0.01 N HCl in USP dissolution apparatus II. The dispersion test showed that all SMEDDS containing nutraceuticals dispersed spontaneously to form microemulsions after disintegration of capsule shells with globule size in the range of 25 to 200 nm. From all formulations, except that of vitamin K2, >80-90% nutraceuticals dispersed in 5-10 min and there was no precipitation of compounds during the test period of 120 min. Some variation in dispersion of vitamin K2 was observed due to the nature of the material used (vitamin K2 pre-adsorbed onto calcium phosphate). The present report provides a simple and organic cosolvent-free lipid-based SMEDDS for the oral delivery of poorly water-soluble nutraceuticals. Although a 50:50 w/w mixture of lipid to surfactant was used, the lipid content may be increased to 70:30 without compromising the formation of microemulsion.

Authors+Show Affiliations

a College of Pharmacy and Health Sciences, Department of Pharmaceutical Sciences , St. John's University , Queens , NY , USA.a College of Pharmacy and Health Sciences, Department of Pharmaceutical Sciences , St. John's University , Queens , NY , USA.a College of Pharmacy and Health Sciences, Department of Pharmaceutical Sciences , St. John's University , Queens , NY , USA. b Celgene Corporation , Summit , NJ , USA.c ABITEC Corporation , Columbus , OH , USA.a College of Pharmacy and Health Sciences, Department of Pharmaceutical Sciences , St. John's University , Queens , NY , USA.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29254385

Citation

Shah, Ankita V., et al. "Development of Self-microemulsifying Drug Delivery System for Oral Delivery of Poorly Water-soluble Nutraceuticals." Drug Development and Industrial Pharmacy, vol. 44, no. 6, 2018, pp. 895-901.
Shah AV, Desai HH, Thool P, et al. Development of self-microemulsifying drug delivery system for oral delivery of poorly water-soluble nutraceuticals. Drug Dev Ind Pharm. 2018;44(6):895-901.
Shah, A. V., Desai, H. H., Thool, P., Dalrymple, D., & Serajuddin, A. T. M. (2018). Development of self-microemulsifying drug delivery system for oral delivery of poorly water-soluble nutraceuticals. Drug Development and Industrial Pharmacy, 44(6), 895-901. https://doi.org/10.1080/03639045.2017.1419365
Shah AV, et al. Development of Self-microemulsifying Drug Delivery System for Oral Delivery of Poorly Water-soluble Nutraceuticals. Drug Dev Ind Pharm. 2018;44(6):895-901. PubMed PMID: 29254385.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of self-microemulsifying drug delivery system for oral delivery of poorly water-soluble nutraceuticals. AU - Shah,Ankita V, AU - Desai,Heta H, AU - Thool,Prajwal, AU - Dalrymple,Damon, AU - Serajuddin,Abu T M, Y1 - 2017/12/26/ PY - 2017/12/20/pubmed PY - 2018/9/25/medline PY - 2017/12/20/entrez KW - Nutraceutical KW - SMEDDS KW - Tween 80 KW - coenzyme Q10 KW - quercetin KW - self-microemulsifying drug delivery system KW - solubility KW - trans-resveratrol KW - vitamin A KW - vitamin K2 SP - 895 EP - 901 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 44 IS - 6 N2 - The objective of the study was to develop a self-microemulsifying drug delivery system (SMEDDS), also known as microemulsion preconcentrate, for oral delivery of five poorly water-soluble nutraceuticals or bioactive agents, namely, vitamin A, vitamin K2, coenzyme Q10, quercetin and trans-resveratrol. The SMEDDS contained a 1:1 mixture (w/w) of Capmul MCM NF (a medium chain monoglyceride) and Captex 355 EP/NF (a medium chain triglyceride) as the hydrophobic lipid and Tween 80 (polysorbate 80) as the hydrophilic surfactant. The lipid and surfactant were mixed at 50:50 w/w ratio. All three of the SMEDDS components have GRAS or safe food additive status. The solubility of nutraceuticals was determined in Capmul MCM, Captex 355, Tween 80, and the SMEDDS (microemulsion preconcentrate mixture). The solubility values of vitamin A palmitate, vitamin K2, coenzyme Q10, quercetin, and trans-resveratrol per g of SMEDDS were, respectively, 500, 12, 8, 56, and 87 mg. Appropriate formulations of nutraceuticals were prepared and filled into hard gelatin capsules. They were then subjected to in vitro dispersion testing using 250 mL of 0.01 N HCl in USP dissolution apparatus II. The dispersion test showed that all SMEDDS containing nutraceuticals dispersed spontaneously to form microemulsions after disintegration of capsule shells with globule size in the range of 25 to 200 nm. From all formulations, except that of vitamin K2, >80-90% nutraceuticals dispersed in 5-10 min and there was no precipitation of compounds during the test period of 120 min. Some variation in dispersion of vitamin K2 was observed due to the nature of the material used (vitamin K2 pre-adsorbed onto calcium phosphate). The present report provides a simple and organic cosolvent-free lipid-based SMEDDS for the oral delivery of poorly water-soluble nutraceuticals. Although a 50:50 w/w mixture of lipid to surfactant was used, the lipid content may be increased to 70:30 without compromising the formation of microemulsion. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/29254385/Development_of_self_microemulsifying_drug_delivery_system_for_oral_delivery_of_poorly_water_soluble_nutraceuticals_ DB - PRIME DP - Unbound Medicine ER -