Influence of Inclusion Complexation and Skin Microporation on Enhancement of Transdermal Permeation of Raloxifene Hydrochloride
By: Thakkar, Hetal P
.
Contributor(s): Savsani, H. G | Srivastava, P. K.
Publisher: Mumbai Indian Journal of Pharmaceutical Science 2019Edition: Vol. 81(1), Jan-Feb.Description: 22-31p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Indian journal of pharmaceutical sciencesSummary: The aim of the present investigation was to develop an inclusion complex-based hydrogel for transdermal delivery of raloxifene hydrochloride. Inclusion complexation was tried using two types of cyclodextrins, β-cyclodextrin and hydroxypropyl-β-cyclodextrin. Kneading, co-precipitation, solvent evaporation and freeze drying were the methods explored for preparing inclusion complexes. The prepared complexes were characterized using differential scanning calorimetry, Fourier-transform infrared spectroscopy, X-ray powder diffraction and both in vitro and ex vivo drug release studies. Kneading method was found to be the most suitable for preparing the inclusion complexes. Phase solubility studies indicated that β-cyclodextrin gave rise to Bs type of curve while hydroxypropyl-β-cyclodextrin resulted in Ap type of curve. The stability constants (K1:1) obtained for β-cyclodextrin and hydroxypropyl-β-cyclodextrin were 1572 and 2960, respectively. Complexation efficiency of hydroxypropyl-β-cyclodextrin was higher than that of β-cyclodextrin. Differential scanning calorimetry, Fourier-transform infrared spectroscopy and X-ray powder diffraction studies indicated the superiority of hydroxypropyl-β-cyclodextrin for complexing raloxifene hydrochloride. In vitro and ex vivo studies showed that highest drug release occurred from inclusion complex prepared with hydroxypropyl-β-cyclodextrin with a ratio of 1:2.5. Histopathology studies revealed that the developed hydrogel was non-irritant and micropores were clearly visible for the microporated skin.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Not for loan | 2018490 |
The aim of the present investigation was to develop an inclusion complex-based hydrogel for transdermal delivery of raloxifene hydrochloride. Inclusion complexation was tried using two types of cyclodextrins, β-cyclodextrin and hydroxypropyl-β-cyclodextrin. Kneading, co-precipitation, solvent evaporation and freeze drying were the methods explored for preparing inclusion complexes. The prepared complexes were characterized using differential scanning calorimetry, Fourier-transform infrared spectroscopy, X-ray powder diffraction and both in vitro and ex vivo drug release studies. Kneading method was found to be the most suitable for preparing the inclusion complexes. Phase solubility studies indicated that β-cyclodextrin gave rise to Bs type of curve while hydroxypropyl-β-cyclodextrin resulted in Ap type of curve. The stability constants (K1:1) obtained for β-cyclodextrin and hydroxypropyl-β-cyclodextrin were 1572 and 2960, respectively. Complexation efficiency of hydroxypropyl-β-cyclodextrin was higher than that of β-cyclodextrin. Differential scanning calorimetry, Fourier-transform infrared spectroscopy and X-ray powder diffraction studies indicated the superiority of hydroxypropyl-β-cyclodextrin for complexing raloxifene hydrochloride. In vitro and ex vivo studies showed that highest drug release occurred from inclusion complex prepared with hydroxypropyl-β-cyclodextrin with a ratio of 1:2.5. Histopathology studies revealed that the developed hydrogel was non-irritant and micropores were clearly visible for the microporated skin.
Click on an image to view it in the image viewer
There are no comments for this item.