首页|Engineered mucoadhesive microparticles of formoterol/budesonide for pulmonary administration

Engineered mucoadhesive microparticles of formoterol/budesonide for pulmonary administration

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In the present study, a multi-component system comprised of dipalmitylphospatidylcholine (DPPC), Chitosan, Lactose, and L-Leucine was developed for pulmonary delivery. Microparticles were engineered by the spray drying process and the selection of the critical parameters was performed by applying experimental design. The microcarriers with the appropriate size and yield were co-formulated with two active pharmaceutical ingredients (APIs), namely, Formoterol fumarate and Budesonide, and they were further investigated. All formulations exhibited spherical shape, appropriate aerodynamic performance, satisfying entrapment efficiency, and drug load. Their physicochemical properties were evaluated using Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy (FT-IR), and Differential Scanning Calorimetry (DSC). The aerodynamic particle size characterization was determined using an eight-stage Andersen cascade impactor, whereas the release of the actives was monitored in vitro in simulated lung fluid. Additional evaluation of the microparticles' mucoadhesive properties was performed by zeta-potential measurements and ex vivo mucoadhesion study applying a falling liquid film method using porcine lung tissue. Cytotoxicity and cellular uptake studies in Calu-3 lung epithelial cell line were conducted to further investigate the safety and efficacy of the developed formulations.

Pulmonary deliverySpray dryingFormoterolBudesonideMucoadhesion

Andriotis, Eleftherios G.、Bouropoulos, Nikolaos、Panteris, Emmanuel、Akrivou, Melpomeni、Vizirianakis, Ioannis S.、Ahmad, Zeeshan、Fatouros, Dimitrios G.、Monou, Paraskevi Kyriaki

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Aristotle Univ Thessaloniki, Dept Pharm, Div Pharmaceut Technol, Thessaloniki 54124, Greece

Univ Patras, Dept Mat Sci, Patras 26504, Greece

Aristotle Univ Thessaloniki, Sch Biol, Dept Bot, GR-54124 Thessaloniki, Greece

Aristotle Univ Thessaloniki, Dept Pharm, Div Pharmacol, Thessaloniki 54124, Greece

De Montfort Univ, Leicester Sch Pharm, Leicester LE1 9BH, Leics, England

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2021

European journal of pharmaceutical sciences

European journal of pharmaceutical sciences

ISTP
ISSN:0928-0987
年,卷(期):2021.165
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