Development and optimization of boswellic acid-loaded proniosomal gel

Abstract

Context: Boswellic acids (BAs) are isolated from oleo gum of Boswellia serrata and are mainly used as potential anti-inflammatory, hypolipidemic, immunomodulatory, and antitumor agents. Pharmacokinetic investigations of BAs uncover its poor bioavailability through digestive system thus creates a need for improved therapeutic responses which can possibly be achieved by developing formulations through novel delivery system. Objective: Present study was conducted to design topical BA-loaded proniosomal gel for the management of inflammatory disorders with enhanced bioavailability. Materials and methods: Nonionic surfactant vesicles were prepared using the coacervation phase separation method. A central composite design was employed to statistically optimize formulation variables using Design-Expert software. Three independent variables were evaluated: amount of surfactant (X 1 ), amount of soya lecithin (X 2 ), and amount of cholesterol (X 3 ). The encapsulation efficiency percentage (Y 1 ) and particle size (Y 2 ) were selected as dependent variables. Results and discussion: The optimum formulation (F10) displayed spherical bi-layered vesicles under transmission electron microscopy with optimum particle size of 707.9 nm and high entrapment efficiency as 98.52%. In vitro skin permeation study demonstrated the most sustained release of 84.83 ± 0.153 mg/cm 2 in 24 h. Anti-inflammatory activity of the gel showed a significant (p 5 0.001) higher percentage inhibition as compared to the marketed gel at the same dose. Conclusion: The present study exhibited that BA-loaded proniosomal gel was better in terms of absorption, bioavailability, and release kinetics.

Proniosomes derived niosomes: recent advancements in drug delivery and targeting

“…Therefore, proniosomes provide a system with high drug entrapment and skin permeation for transdermal delivery of flurbiprofen (Zidan & Mokhtar, 2011). Mehta et al (2016) designed topical boswellic acid (BA) loaded proniosomal gel carrier system to augment its bioavailability, absorption, and release kinetics for the management of inflammatory disorders. Boswellic acid is a leukotriene inhibitor and showed remarkable antiinflammatory effects as compared to standard Voveran gel.…”

“…Boswellic acid is a leukotriene inhibitor and showed remarkable antiinflammatory effects as compared to standard Voveran gel. Furthermore, transdermal delivery is enhanced due to small particle size and significant encapsulation of drugs within vesicles (Mehta et al, 2016). Similarly, the topical drug delivery system of Tretinoin loaded proniosomes were designed by Rahman et al (2015) to improve the effectiveness of tretinoin by minimizing its side effects for acne treatment.…”

<p>Formulation of Nanospanlastics as a Promising Approach for ‎Improving the Topical Delivery of a Natural Leukotriene Inhibitor (3-‎Acetyl-11-Keto-β-Boswellic Acid): Statistical Optimization, in vitro ‎Characterization, and ex vivo Permeation Study</p>

“…Moreover, AKBA is significantly affected by the hepatic first-pass effect that reduces its systemic absorption. 8 Furthermore, reducing inflammation required a high concentration of AKBA at the site of inflammation. Thus topical delivery of AKBA seems to be a preferred alternative to an oral dosage form, which could be directly applied to the target tissues reducing the frequency of administration and increasing drug efficiency.…”

Formulation and in Vitro, in Vivo Evaluation of Proniosomal Gel of Neomycin Sulphate

“…niosomes that overcomes several of these problems associated with liposomes [3]. Non-ionic surfactant vesicles obtained on hydration of synthetic non-ionic surfactants, with or without incorporation of cholesterol or other lipid [4]. But the proniosomes are more advantageous than nonionic surfactant vesicles i.e., niosomes, in terms of physical stability such as aggregation, fusion and leaking, and provide additional convenience in transportation, distribution, storage, and dosing [5].…”