TY - JOUR
T1 - Solid-state properties, solubility, stability and dissolution behaviour of co-amorphous solid dispersions of baicalin
AU - Jangid, Ashok Kumar
AU - Jain, Poonam
AU - Medicherla, Kanakaraju
AU - Pooja, Deep
AU - Kulhari, Hitesh
N1 - Publisher Copyright:
© The Royal Society of Chemistry 2020.
PY - 2020/10/7
Y1 - 2020/10/7
N2 - Baicalin (BL) is a natural, potential therapeutic molecule with a wide range of biological activities. However, poor aqueous solubility, low stability, and slow dissolution are the major limitations of BL. Co-amorphous systems are new and emerging systems that are single-phase, multicomponent amorphous systems consisting of one or more small co-former with a hydrophobic drug. The co-former helps in improving the physicochemical properties of the hydrophobic drug without affecting its pharmacological properties. The objective of this study was to prepare co-amorphous solid dispersions of baicalin (BSDs) using organic acids and amino acids to enhance its solubility, stability and dissolution profiles. The BSDs were prepared in a molar ratio of 1 : 1 of drug and co-former by the solvent evaporation method. The prepared BSDs were characterized by powder XRD and DSC analysis for determining the physical solid-state of BL, and by FTIR to determine possible intermolecular interactions between BL and co-formers. The BSD prepared with histidine (BL-His) showed a perfect co-amorphous system with an approximately 60-fold increase in solubility, complete loss of crystallinity, and complete dissolution of BL within 15 min in simulated intestinal buffer. Further, BL-His showed physicochemical stability over a period of six months without any sign of recrystallization and loss of drug. Therefore, instead of the native and crystalline BL, the use of BL-His could be a better approach for pharmaceutical applications of BL.
AB - Baicalin (BL) is a natural, potential therapeutic molecule with a wide range of biological activities. However, poor aqueous solubility, low stability, and slow dissolution are the major limitations of BL. Co-amorphous systems are new and emerging systems that are single-phase, multicomponent amorphous systems consisting of one or more small co-former with a hydrophobic drug. The co-former helps in improving the physicochemical properties of the hydrophobic drug without affecting its pharmacological properties. The objective of this study was to prepare co-amorphous solid dispersions of baicalin (BSDs) using organic acids and amino acids to enhance its solubility, stability and dissolution profiles. The BSDs were prepared in a molar ratio of 1 : 1 of drug and co-former by the solvent evaporation method. The prepared BSDs were characterized by powder XRD and DSC analysis for determining the physical solid-state of BL, and by FTIR to determine possible intermolecular interactions between BL and co-formers. The BSD prepared with histidine (BL-His) showed a perfect co-amorphous system with an approximately 60-fold increase in solubility, complete loss of crystallinity, and complete dissolution of BL within 15 min in simulated intestinal buffer. Further, BL-His showed physicochemical stability over a period of six months without any sign of recrystallization and loss of drug. Therefore, instead of the native and crystalline BL, the use of BL-His could be a better approach for pharmaceutical applications of BL.
UR - http://www.scopus.com/inward/record.url?scp=85091962940&partnerID=8YFLogxK
U2 - 10.1039/d0ce00750a
DO - 10.1039/d0ce00750a
M3 - Article
AN - SCOPUS:85091962940
SN - 1466-8033
VL - 22
SP - 6128
EP - 6136
JO - CrystEngComm
JF - CrystEngComm
IS - 37
ER -