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.
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 -
