Abstract
Objective: The present work was aimed to prepare niosomes entrapping salbutamol sulphate (SS) using reversed phase evaporation method (REV).Methods: Niosomes were prepared by mixing span 60 and cholesterol in 1:1 molar ratio in chloroform, SS in water was then added to organic phase to form niosomal SS. Formulations after evaporation of chloroform, freeze centrifuged then lyophilized, were evaluated for particles size, polydispersity index (Pdi), zeta-potential, morphology, entrapment efficiency (EE%) and in vitro release. For pulmonary delivery; metered dose inhalers (MDI) were prepared by suspending SS niosomes equivalent to 20 mg SS in hydrofluoroalkane (HFA). The metered valve was investigated for leakage rate, the total number of puffs/canister, weight/puff, dose uniformity and particle size.Results: The results showed spherical niosomes with 400-451 nm particles that entrapped 66.19% of SS. 76.54±0.132% SS release from niosomes that showed a controlled release profile for 8h. The leakage test was not exceeding 4 mg/3 d, the number of puffs were up to 200puffs/canister, the dose delivered/puff was 0.1 mg and 0.64-4.51μm niosomal aerosol.Conclusion: The results indicate an encouraging strategy to formulate a controlled drug delivery by entrapping (SS) in niosomes which could be packaged into (MDI) that met the requirements of (USP) aerosols guidelines which offering a novel approach to respiratory delivery.
Highlights
The pulmonary delivery route is characterized with rapid onset, non-invasive nature and lack of proteolytic enzymes in lungs compared to gastrointestinal tract
Reversephase evaporation method has these unique advantages for encapsulating water-soluble materials such salbutamol sulphate (SS) as the organic solvent is removed from the inverted micelles resulting in vesicles with larger aqueous space to lipid ratio and higher EE%
Polydispirsity index (Pdi) value was 0.354 that indicates the homogenous distribution of formed niosomes
Summary
The pulmonary delivery route is characterized with rapid onset, non-invasive nature and lack of proteolytic enzymes in lungs compared to gastrointestinal tract. Salbutamol sulphate (SS) was developed and indicated for the symptomatic relief and prevention of bronchospasm due to bronchial asthma, chronic bronchitis and other chronic Broncho pulmonary disorders in which bronchospasm is a complicating factor. Anti-asthmatic drugs have high potential to induce toxic side effects after parenteral administration; stimulation of beta receptors, occur in the body. This effect results in cardiac stimulation by receptors and peripheral vasodilatation and hypotension [11]. The aforementioned facts directed our interest to design a new nano-based SS MDI according to the USP guidelines to reduce the uptake of SS by β1 receptors and to deliver the drug in a controlled manner which reduces the recurrent doses and reduces its toxic effect
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