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Enhanced solubility of piperine using hydrophilic carrier-based potent solid dispersion systems.
Drug Dev Ind Pharm. 2017 Sep; 43(9):1501-1509.DD

Abstract

CONTEXT

Piperine alkaloid, an important constituent of black pepper, exhibits numerous therapeutic properties, whereas its usage as a drug is limited due to its poor solubility in aqueous medium, which leads to poor bioavailability.

OBJECTIVE

Herein, a new method has been developed to improve the solubility of this drug based on the development of solid dispersions with improved dissolution rate using hydrophilic carriers such as sorbitol (Sor), polyethylene glycol (PEG) and polyvinyl pyrrolidone K30 (PVP) by solvent method. Physical mixtures of piperine and carriers were also prepared for comparison.

METHODS

The physicochemical properties of the prepared solid dispersions were examined using SEM, TEM, DSC, XRD and FT-IR. In vitro dissolution profile of the solid dispersions was recorded and compared with that of the pure piperine and physical mixtures. The effect of these carriers on the aqueous solubility of piperine has been investigated.

RESULTS

The solid dispersions of piperine with Sor, PEG and PVP exhibited superior performance for the dissolution of piperine with a drug release of 70%, 76% and 89%, respectively after 2 h compared to physical mixtures and pure piperine, which could be due to its transformation from crystalline to amorphous form as well as the attachment of hydrophilic carriers to the surface of poorly water-soluble piperine.

CONCLUSION

Results suggest that the piperine solid dispersions prepared with improved in vitro release exhibit potential advantage in delivering poorly water-soluble piperine as an oral supplement.

Authors+Show Affiliations

a Department of Chemistry , School of Advanced Sciences, VIT University , Vellore , Tamil Nadu , India.b School of Chemical and Biological Engineering, Seoul National University , Seoul , Republic of Korea.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28425323

Citation

Thenmozhi, Kathavarayan, and Young Je Yoo. "Enhanced Solubility of Piperine Using Hydrophilic Carrier-based Potent Solid Dispersion Systems." Drug Development and Industrial Pharmacy, vol. 43, no. 9, 2017, pp. 1501-1509.
Thenmozhi K, Yoo YJ. Enhanced solubility of piperine using hydrophilic carrier-based potent solid dispersion systems. Drug Dev Ind Pharm. 2017;43(9):1501-1509.
Thenmozhi, K., & Yoo, Y. J. (2017). Enhanced solubility of piperine using hydrophilic carrier-based potent solid dispersion systems. Drug Development and Industrial Pharmacy, 43(9), 1501-1509. https://doi.org/10.1080/03639045.2017.1321658
Thenmozhi K, Yoo YJ. Enhanced Solubility of Piperine Using Hydrophilic Carrier-based Potent Solid Dispersion Systems. Drug Dev Ind Pharm. 2017;43(9):1501-1509. PubMed PMID: 28425323.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhanced solubility of piperine using hydrophilic carrier-based potent solid dispersion systems. AU - Thenmozhi,Kathavarayan, AU - Yoo,Young Je, Y1 - 2017/05/05/ PY - 2017/4/21/pubmed PY - 2017/9/29/medline PY - 2017/4/21/entrez KW - Piperine KW - hydrophilic carriers KW - polyethylene glycol KW - polyvinyl pyrrolidone K30 KW - solid dispersion KW - solubility SP - 1501 EP - 1509 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 43 IS - 9 N2 - CONTEXT: Piperine alkaloid, an important constituent of black pepper, exhibits numerous therapeutic properties, whereas its usage as a drug is limited due to its poor solubility in aqueous medium, which leads to poor bioavailability. OBJECTIVE: Herein, a new method has been developed to improve the solubility of this drug based on the development of solid dispersions with improved dissolution rate using hydrophilic carriers such as sorbitol (Sor), polyethylene glycol (PEG) and polyvinyl pyrrolidone K30 (PVP) by solvent method. Physical mixtures of piperine and carriers were also prepared for comparison. METHODS: The physicochemical properties of the prepared solid dispersions were examined using SEM, TEM, DSC, XRD and FT-IR. In vitro dissolution profile of the solid dispersions was recorded and compared with that of the pure piperine and physical mixtures. The effect of these carriers on the aqueous solubility of piperine has been investigated. RESULTS: The solid dispersions of piperine with Sor, PEG and PVP exhibited superior performance for the dissolution of piperine with a drug release of 70%, 76% and 89%, respectively after 2 h compared to physical mixtures and pure piperine, which could be due to its transformation from crystalline to amorphous form as well as the attachment of hydrophilic carriers to the surface of poorly water-soluble piperine. CONCLUSION: Results suggest that the piperine solid dispersions prepared with improved in vitro release exhibit potential advantage in delivering poorly water-soluble piperine as an oral supplement. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/28425323/Enhanced_solubility_of_piperine_using_hydrophilic_carrier_based_potent_solid_dispersion_systems_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639045.2017.1321658 DB - PRIME DP - Unbound Medicine ER -