Preparation of honokiol-loaded chitosan microparticles via spray-drying method intended for pulmonary delivery

Abstract

R E S E A R C H A R T I C L EPreparation of honokiol-loaded chitosan microparticles via spray-drying method intended for pulmonary delivery IntroductionAt present, many drugs in clinic have to be administered by injection because of its poor oral bioavailability. However, injection route is not convenient for the patients due to poor compliance, pain, and etc. In the search for needle-free delivery, the administration of therapeutic drugs by inhalation is a promising alternative that has gained considerable interest over the past few years (Smith, 1997;Bosquillon et al., 2004). The lung was an attractive route for drug delivery because it was an efficient portal to the bloodstream, and it also could be the target organ. Besides, the lung could offer large absorptive surface area in the range of 35-140 m 2 , and thin (0.2 µm) and highly vascularized epithelium, which could lead to high bioavailability (Shoyele and Cawthorne, 2006). Moreover, inhalation is well accepted by the general population because of the convenience and good compliance (Byron, 1990).Preparation of dry powder formulations for inhalation is an attractive and appreciated proposal because solubility and stability issues of drugs can be resolved. Furthermore, a dry powder aerosol offers the capacity to provide a wide range of single dose per inhalation. The success of inhaled particles mostly depends on their size and density, and especially aerodynamic diameter (d ae ) (Grenha et al., 2005). Generally, the powder with aerodynamic diameter ranging from 1-5 µm could guarantee a maximum deposition in the deep lung. Particles size smaller than 1 µm failed to deposit in lung because it was easily breathed out again, and particle sizes larger than 5 µm also failed to deposit in the lung because they could not pass through the upper airways and cannot reach the deep lung (Broadhead et al.,1992;Bosquillon et al., 2001).Micronization is usually adopted to reduce the particle size of powder to less than 5 µm. Traditional method of micronization was using a ball or jet mill to produce powder. Whereas milling is a destructive Abstract It has been demonstrated that spray-drying is a powerful method to prepare dry powders for pulmonary delivery. This paper prepared dispersible dry powders based on chitosan and mannitol containing honokiol nanoparticles as model drug. The results showed that the prepared microparticles are almost spherical and have appropriate aerodynamic properties for pulmonary delivery (aerodynamic diameters was between 2.8-3.3 μm and tapped density ranging from 0.14-0. 18 g/cm 3 ). Moreover, surface morphology and aerodynamic properties of the powders were strongly affected by the content of mannitol. Fourier transform infra-red (FTIR) spectrum of powders indicated that the honokiol nanoparticles were successfully incorporated into microparticles. In vitro drug release profile was also observed. The content of mannitol in powders significantly influenced the release rate of honokiol from matrices. Keywords: Honokiol nanoparticles; spray-d...

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