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Inclusion Complexes of Hydroxy Propyl-β-Cyclodextrin and Paliperidone: Preparation and Characterization
In the present investigation an attempt has been made to improve aqueous solubility of a BCS class II drug by making an inclusion complex with Hydroxypropyl-β-cyclodextrin (HP-β-CD). Paliperidone (PALI) was selected as a model drug for the study. It is practically insoluble in water with low oral bioavailability. It is a major active metabolite of risperidone approved for the treatment of schizophrenia in adults. The inclusion complexes were prepared in 1:1 (PALI: HP-β-CD) molar ratio. Phase solubility studies were performed according to Higuchi Connors method to determine the optimum conditions for the complexation. The prepared solid inclusion complexes were characterized by Differential Scanning Calorimetry (DSC) Fourier- Transform Infrared Spectroscopy (FT-IR) Powder X-ray Diffractometry (PXRD) Scanning Electron Microscopy (SEM) and Proton Nuclear Magnetic Resonance Spectroscopy (1H-NMR). Dissolution study was performed using USP apparatus II in phosphate buffer pH 6.8 (37 ± 0.5°C). The solid state characterization studies confirmed the formation of inclusion complex between PALI and HP-β-CD. The aqueous solubility and in-vitro dissolution study showed that the solubility and dissolution rate of drug were considerably improved by complexation with HP-β-CD with respect to the drug alone. The enhanced solubility and dissolution may help to improve in-vivo performance of PALI. Thus the binary complexation of PALI with HP-β-CD can be used as an approach for its solubility enhancement.
Proliposomes for Oral Delivery: Progress and Challenges
Proliposomes are phospholipid based drug delivery systems that are finding important applications in the field of pharmaceutics. Proliposomes have been extensively studied as a potential carrier for oral delivery of drugs with poor bioavailability but the mechanism of absorption and cellular uptake pathways has not yet been clearly understood. An in-depth insight into the physical and biological behavior of proliposomes is necessary for designing an effective delivery system for enhancing the availability of drug at the intended site. Reformulation of sub optimal drugs using proliposomes has given an opportunity to improve the therapeutic indices of various drugs predominantly by altering their uptake mechanism. This work reviews the proliposomal drug delivery field summarizes the success of proliposomes for the oral delivery of drugs with poor bioavailability; indicating the key issues to be addressed to affirm that proliposomes can effectively work as a drug carrier in clinical settings with a clear understanding of its behavior in biological environment as they are now an established platform technology with considerable clinical acceptance.