Dewi Melani Hariyadi, - (2018) Development of Alginate-Based Microspheres for Lung Delivery In Cystic Fibrosis. Laporan Penelitian. UNIVERSITAS AIRLANGGA, SURABAYA.

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Abstract

Cystic Fibrosis affects about one out of every 3,000 Ht:wbofllS aUlI abuut um: iu 25 people are carriers, including in Africans anu Asialls. Cystic.: Fibrosis is a genetic disorder that affects lIIusLly the lungs. Lung infections arc treated with antibiotics which may be given intravenously, inhaled, or by mouth. Sometimes the antibiotic is used long tcnn. Lung transplantation may be an option if lung function continues to worsen. Lung problems are responsible for death in 80% of people with cystic tibrosis. Inhalation treatment using antibiotic is an alternative for lung delivery especially for cystic fibrosis, however, the therapeutic efficacy of inhaled drugs is limited by their rapid clearance in the lungs. Sustained release system in the lungs can improve therapeutic outcomes of inhaled drugs because they can retain the drug load within the lungs and progressively release the drug locally at therapeutic levels. This study presents the fonnulation strategies developed to control drug release in the lungs using microspheres system. Microspheres are carrier for sustained drug release in the lungs which offer significant potential for prolonged drug release in the lungs. The microspheres composition can be adjusted to modulate drug release and can encapsulate compounds with high drug loading. Pulmonary route is commonly used and has been well accepted as a portal for non-invasive drug delivery for many lung diseases and it is explored for decades as an alternative for systemic as well as local drug delivery. The pharmaceutical scientists are taking advantage of large peripheral surface area of lung for absorption and thinner alveolar epitheliuUl providing shorter distance of air-blood exchange passage. Alginate-based microspheres provide sustained release properties with several advantages such as minimum usage of toxic organic solvents and reduced reticuloendothelial systcm uptake due to stealth nature of alginate. The present study explores the in vitro benefits of antibiotic encapsulated alginate microspheres. The encapsulation method is by aerosolization technique considered as simple, easy, and produces small and uniform particle size. The present study was to evaluate optimized a natural polymer-based inhalable drug delivery system using sodium alginate and antibiotic ciprofloxacin as a model. Small, good, smooth and spherical microspheres were found. In vitro release study showed sustained release profile was achieved; this is potential for pulmonary delivery. The antimicrobial potency against microorganism in lung disease was also effectively found. Stability of microspheres which stored at room temperature was found stable and able to maintain concentrations of antibiotic, however at high temperature, ciproflocain HCI-alginate microspheres were found stable for 21 days storage. Conducting long term stability test and in vivo study are highly recommended for further study. iii

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