Abstract
Objective: The main objective of the present study was to develop proniosomal formulations to enhance the oral bioavailability of rosuvastatin calcium by improving solubility, dissolution, and/or intestinal permeability.
 Methods: Proniosomal powder formulations were prepared with rosuvastatin calcium drug varying the Span 40 and cholesterol ratio in the range of 0.8:0.2–0.2:0.8 using maltodextrin as 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: Physicochemical studies help in optimization of formulations. Enhancement in dissolution is due to incorporation of rosuvastatin calcium 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 gastrointestinal membrane compared to control.
 Conclusion: Proniosomes provide a powerful and functional way of distribution of inadequately soluble rosuvastatin calcium drug which is proved from in vivo studies based on the enhanced oral delivery.
Highlights
Enhancement in dissolution is due to incorporation of rosuvastatin calcium into the non-ionic surfactant and change in the physical state from crystalline to amorphous, improving oral bioavailability
Proniosomes provide a powerful and functional way of distribution of inadequately soluble rosuvastatin calcium drug which is proved from in vivo studies based on the enhanced oral delivery
The rosuvastatin calcium proniosomes were prepared by slurry method using maltodextrin as carrier at varying ratios of Spans and cholesterol
Summary
The conventional techniques of improving the bioavailability act by enhancing the dissolution behavior [1] such as reducing the particle size by cogrinding technique [2], in situ crystallization [3], spray drying technique [4] but cannot preclude or alter the gastrointestinal tract barrier function and pre-systemic metabolism along with particulate aggregates formation, and toxicity from vehicles [5,6]. To overcome all such difficulties encapsulation of the drug in vesicular structures [7] in the form of pharmacosomes, liposomes [8], niosomes [9], and cubosomes 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]. With benefits of firmness during sterilization, measuring, transfer, distribution, and storage proniosomes became a versatile system for delivery of numerous drugs [18,19]
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