Abstract
Objective: The main objective of the present study was to develop proniosomal formulations to enhance the oral bioavailability of bazedoxifene acetate by improving solubility, dissolution and/or intestinal permeability.
 Methods: Proniosomal powder formulations were prepared with bazedoxifene acetate drug varying the span 40 and cholesterol ratio in the range of 0.8:0.2 to 0.2:0.8 using maltodextrin as a carrier by slurry method. The prepared proniosomal powder was filled into capsules. The bioavailability enhancement of proniosomes loaded with drug was studied focusing on non-ionic surfactants composition and drug: span 40 ratio. Prepared proniosomes were characterized for their particle size distribution, zeta potential, entrapment efficiency, in vitro dissolution study and thermal characteristics to understand the phase transition behavior. Further, the formulated proniosomes were subjected to stability behavior, ex vivo permeation studies using rat intestine followed by in vivo studies.
 Results: Physico-chemical studies help in the optimization of formulations. Enhancement in dissolution is due to the incorporation of bazedoxifene acetate into the non-ionic surfactant and change in the physical state from crystalline to amorphous, thus improving oral bioavailability. Ex vivo studies show significant permeation enhancement across the gastrointestinal membrane compared to control.
 Conclusion: In conclusion, proniosomes provide a powerful and functional way of the distribution of inadequately soluble bazedoxifene acetate drug, which is proved from in vivo studies based on the enhanced oral delivery.
Highlights
The improvement of oral extent of absorption for poorly or inadequately aqueous soluble active pharmaceutical ingredient is still the most crucial and demanding feature in the development of dosage forms
To overcome all such difficulties encapsulation of the drug in vesicular structures [7] in the form of pharmacosomes, liposomes [8], niosomes [9], cubosomes, transferosomes are one such system, which can be expected to prolong the duration of the drug in systemic circulation, and reduce the toxicity by selective uptake along with lymphatic transport leading to improved permeation [10] along with rate and extent of absorption by avoidance of first pass metabolism [11]
Acquired proniosome powders are kept in glass vial at 4 °C, which can be delivered in the form of capsules
Summary
The improvement of oral extent of absorption for poorly or inadequately aqueous soluble active pharmaceutical ingredient is still the most crucial and demanding feature in the development of dosage forms. To overcome all such difficulties encapsulation of the drug in vesicular structures [7] in the form of pharmacosomes, liposomes [8], niosomes [9], cubosomes, transferosomes are one such system, which can be expected to prolong the duration of the drug in systemic circulation, and reduce the toxicity by selective uptake along with lymphatic transport leading to improved permeation [10] along with rate and extent of absorption by avoidance of first pass metabolism [11]. Niosomes [12] which are comparitively stable chemically and cheap in price because of usage of surfactants instead of phospholipids used in liposomes face physico-stability problems namely sedimentation of particles leading to fusion and aggregation and leakage of drug upon storage
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