Solid lipid microparticles as a sustained release system for pulmonary drug delivery

Jaspart, Séverine; Bertholet, Pascal; Piel, Géraldine; Dogné, Jean‐Michel; Delattre, Luc; Évrard, Brigitte

doi:10.1016/j.ejpb.2006.07.006

Cited by 114 publications

(62 citation statements)

References 30 publications

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“…In one previous study, Jaspart et al studied the release of a model drug, salbutamol acetonide, from a glycerol behenate-based solid lipid system (11). Although, in this previous study, the microparticles were of a suitable size for inhalation therapy, the aerosol performance was not studied.…”

Section: Introductionmentioning

confidence: 99%

Solid Lipid Budesonide Microparticles for Controlled Release Inhalation Therapy

Mezzena

Scalia

Young

et al. 2009

AAPS J

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Abstract. A solid lipid microparticle system containing budesonide was prepared by oil in water emulsification followed by spray drying. The solid lipid system was studied in terms of morphology, particle size distribution, crystallinity, thermal properties, aerosol performance, and dissolution/diffusion release. The microparticle system was also compared to conventional spray-dried crystalline and amorphous budesonide samples. The particle size distributions of the crystalline, amorphous, and solid lipid microparticles, measured by laser diffraction, were similar; however, the microparticle morphology was more irregular than the spray-dried drug samples. The thermal response of the solid lipid microparticles suggested polymorphic transition and melting of the lipid, glycerol behenate (at~48°C and 72°C). No budesonide melting or crystallisation peaks were observed, suggesting that the budesonide was integrated into the matrix. X-ray powder diffraction patterns of the crystalline and amorphous budesonide were consistent with previous studies while the solid lipid microparticles showed two peaks, at approximately 21.3 and 23.5 2θ suggesting the metastable sub-α and primarily β′ form. Analysis of the in vitro diffusion/dissolution of the formulations was studied using a flow through model and curves analysed using difference/similarity factors and fitted using the Higuchi model. Regression analysis of this data set indicated differences in the t 0.5 , where values of 49.7, 35.3, and 136.9 min were observed for crystalline, amorphous, and the solid lipid microparticles, respectively. The aerosol performance (<5 μm), measured by multistage liquid impinger, was 29.5%, 27.3%, and 21.1±0.6% for the crystalline, amorphous, and the solid lipid microparticles, respectively. This study has shown that solid lipid microparticles may provide a useful approach to controlled release respiratory therapy.

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Section: Introductionmentioning

confidence: 99%

Solid Lipid Budesonide Microparticles for Controlled Release Inhalation Therapy

Mezzena

Scalia

Young

et al. 2009

AAPS J

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“…Over the past few years many different drugs had been successfully incorporated in lipid nano-or microparticles [20,[26][27][28]. Relatively higher drug encapsulation efficiency was one of the major advantages of lipid nanoparticles.…”

Section: Drug Entrapment Efficiency and Loading Capacitymentioning

confidence: 99%

“…Emulsion formation and solvent evaporation method has been widely used for particle formation, although other methods like high pressure homogenization [18], solvent diffusion methods in aqueous solutions [19] or hot emulsion methods [18,20] have also been employed. Drawbacks associated to this kind of formulations, like limited drug loading capacity, adjustment of drug release profile and potential drug expulsion during storage have been reported [21].…”

Section: Introductionmentioning

confidence: 99%

Lipid nanoparticles for alkyl lysophospholipid edelfosine encapsulation: Development and in vitro characterization

Mendoza

Rayo

Mollinedo

et al. 2008

European Journal of Pharmaceutics and Biopharmaceutics

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The ether lipid 1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphocholine, edelfosine ) is the prototype molecule of a promising class of antitumour drugs named alkyl-lysophospholipid analogues (ALPs) or antitumor ether lipids. This drug presents a very important drawback as can be the dose depending haemolysis when administered intravenously. Lipid nanoparticles have been lately proposed for different drug encapsulation as an alternative to other controlled release delivery systems, such as liposomes or polymeric nanoparticles. The aim of this study was to develop a lipid nanoparticulate system that would decrease systemic toxicity as well as improve the therapeutic potential of the drug. Lipids employed were Compritol ® 888 ATO and stearic acid. The nanoparticles were characterized by photon correlation spectroscopy for size and size distribution, and atomic force microscopy (AFM) was used for the determination of morphological properties. By both differential scanning calorimetry (DSC) and X-ray diffractometry, crystalline behaviour of lipids and drug was assessed.The drug encapsulation efficiency and the drug release kinetics under in vitro conditions were measured by HPLC-MS. It was concluded that Compritol ® presents advantages as a matrix material for the manufacture of the nanoparticles and for the controlled release of edelfosine.

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“…Compared with other carriers such as liposomes and microparticles, SLMs combine several of those carriers' advantages (possibility of controlled drug release and drug targeting), while avoiding some of their disadvantages such as the use of organic solvent, biotoxicity of the carrier system, chemical and physical storage instability for both the carrier and the drug, high cost of ingredients, difficulty in preparation and low scale-up potential [8][9][10][11]. Uronnachi et al developed and characterized AZT-based SLM for control delivery [12] and demonstrated their safety and efficacy of lipid-based carriers that make them potential alternative drug carrier materials to polymers.…”

Section: Introductionmentioning

confidence: 99%