Preparation, characteristic and pharmacological study on inclusion complex of sulfobutylether-β-cyclodextrin with glaucocalyxin A.
OBJECTIVE
The objective of this study was to improve the water solubility and solubility of glaucocalyxin A (GLA) by producing its inclusion complex with sulfobutylether-β-cyclodextrin (SBE-β-CD).


METHODS
The formation of its 1:1 complex with SBE-β-CD in solution was confirmed by phase-solution and spectral-shift studies. The interaction of GLA and SBE-β-CD was examined by differential scanning calorimetry, powder X-ray diffraction, Fourier transform infrared spectroscopy, proton nuclear magnetic resonance spectroscopy and ultraviolet-visible spectroscopy to determine the formation of the GLA-SBE-β-CD inclusion complex.


RESULTS
The solubilities of GLA and its complexes were 2.38 × 10(2) and 1.82 × 10(4)  μg/ml, respectively, and the values of the inclusion complexes were significantly improved by 76-fold compared with the solubility of free GLA. Moreover, a higher area under the curve0-∞ after inclusion technique was observed in the pharmacokinetics study.


CONCLUSIONS
The aforementioned results indicate that GLA-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery.
School of Pharmaceutical Sciences, Nanjing University of Technology, Nanjing, China.
Lili
L
Ren
Jianghui
J
Jing
Guoguang
G
Chen
Yanfei
Y
Miao
Ping
P
Wei
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D019540:Area Under Curve; D002152:Calorimetry, Differential Scanning; D045786:Diterpenes, Kaurane / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D008297:Male; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013057:Spectrum Analysis / Q000379:methods; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000737:chemistry*
D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D045786:Diterpenes, Kaurane; D004337:Drug Carriers; D047392:beta-Cyclodextrins; C093196:SBE4-beta-cyclodextrin; C055124:glaucocalyxin A
characterization; cyclodextrin; glaucocalyxin A; inclusion complex