2011
DOI: 10.1016/j.jconrel.2010.10.034
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Nanonization of megestrol acetate by laser fragmentation in aqueous milieu

Abstract: Nanonization is a simple and effective method to improve dissolution rate and oral bioavailability of drugs with poor water solubility. There is growing interest to downscale the nanocrystal production to enable early preclinical evaluation of new drug candidates when compound availability is scarce. The purpose of the present study was to investigate laser fragmentation to form nanosuspensions in aqueous solution of the insoluble model drug megestrol acetate (MA) using very little quantities of the drug. Lase… Show more

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Cited by 64 publications
(55 citation statements)
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“…Nevertheless, work in progress for other hydrophobic drugs, such as megesterol acetate, suggests that fs laser fragmentation may be an alternative route for the production of nanoparticles of other poorly water soluble and less sensitive drugs. 26 Finally, another current limitation of the fs technique as presented here is that the efficiency of the process is limited by the increase in turbidity of the suspension as more particles are produced. However, this problem could be easily solved by implementing a continuous flow system, which may also eventually lead to lower degradation of the drug.…”
Section: Resultsmentioning
confidence: 97%
“…Nevertheless, work in progress for other hydrophobic drugs, such as megesterol acetate, suggests that fs laser fragmentation may be an alternative route for the production of nanoparticles of other poorly water soluble and less sensitive drugs. 26 Finally, another current limitation of the fs technique as presented here is that the efficiency of the process is limited by the increase in turbidity of the suspension as more particles are produced. However, this problem could be easily solved by implementing a continuous flow system, which may also eventually lead to lower degradation of the drug.…”
Section: Resultsmentioning
confidence: 97%
“…The cogrinding technique can reduce particles to the submicron level and a stable amorphous solid can be obtained [12]. [19,20]. We have the following.…”
Section: Dry Cogrindingmentioning
confidence: 99%
“…Secondly, viral sanctuaries breed resistance and often include the brain and lymphatics. These may be targeted by loading nanoparticulate [19,60] drug into macrophages which target these organs, increasing antiviral drug concentration in these typically inaccessible regions. Finally, a strategy for dendritic cell vaccines has been developed for use against bioweapons [63].…”
Section: Nanosuspension Formulations For Treating Bioweaponmediated Dmentioning
confidence: 99%
“…However, 40% to 70% of newly-discovered chemical entities for use in pharmaceuticals are poorly soluble in water. This solubility problem is one of the main causes of difficulties with delivering existing drugs, and represents an obstacle for formulation scientists [1][2][3][4]. Low solubility leads to decreased bioavailability, incomplete release from formulation and limited possibilities in choosing delivery technologies.…”
Section: Introductionmentioning
confidence: 99%