Drug nanocrystals for the formulation of poorly soluble drugs and its application as a potential drug delivery system

Gao, Lei; Zhang, Dianrui; Chen, Ming‐Hui

doi:10.1007/s11051-008-9357-4

Cited by 340 publications

(194 citation statements)

References 53 publications

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“…concentration of Tween 80 was fixed to 1%w/v as it was found that zeta potential of NCH3 was -36.79 mV which is expected to be a stable formulation according to the literature. 18 The selected batches from first generation approach using specific concentration of stabilizers, which showed optimum particle size, were subjected to second generation process (H96 process). The particle size, PDI and zeta potential of nanosuspensions prepared by H96 process were summarized in Table 4.…”

Section: Discussionmentioning

confidence: 99%

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

S¹,

Deshpande²,

Attari³

et al. 2016

Adv Pharm Bull

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Section: Discussionmentioning

confidence: 99%

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

S¹,

Deshpande²,

Attari³

et al. 2016

Adv Pharm Bull

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“…This method however requires that an appropriate pair of solvent/antisolvent is established and their ratio optimized for each compound, which is certainly a shortcoming in a tight drug supply context. Moreover, amorphous nanoparticles may result from this process and the organic solvents used should be eliminated from the formulation to avoid toxic effects [14].…”

Section: Introductionmentioning

confidence: 99%

Nanonization of megestrol acetate by laser fragmentation in aqueous milieu

Sylvestre

Tang

Fürtös

et al. 2011

Journal of Controlled Release

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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. Laser fragmentation was obtained by focusing a femtosecond (fs) or nanosecond (ns) laser radiation on a magnetically stirred MA suspension in water or aqueous solution of a stabilizing agent. The size distribution and physicochemical properties of the drug nanoparticles were characterized, and the in vitro dissolution and in vivo oral pharmacokinetics of a laser fragmented formulation were evaluated. A MA nanosuspension was also prepared by media milling for comparison purpose. For both laser radiations, smaller particles were obtained as the laser power was increased, but at a cost of higher degradation. Significant nanonization was achieved after a 30-min fs laser treatment at 250 mW and a 1-h ns laser treatment at 2500 mW. The degradation induced by the laser process of the drug was primarily oxidative in nature. The crystal phase of the drug was maintained, although partial loss of crystallinity was observed. The in vitro dissolution rate and in vivo bioavailability of the laser fragmented formulation were similar to those obtained with the nanosuspension prepared by media milling, and significantly improved compared to the coarse drug powder. It follows that this laser nanonization method has potential to be used for the preclinical evaluation of new drug candidates.

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“…dispersi yang terbentuk bersifat lebih stabil untuk jangka panjang [14]. Potensial zeta dari suatu nanoemulsi digunakan untuk mengkarakterisasi muatan permukaan.…”

Section: P R O O F R E a D I N G V E R S I O Nunclassified

“…Nilai potensial zeta dapat menunjukan kestabilan dari suatu sistem yang mengandung globul-globul terdispersi melalui adanya gaya tolak-menolak antara partikel yang bermuatan sama ketika berdekatan. Nilai potensial zeta yang lebih besar dari (+30) mV atau lebih kecil dari (-30) mV akan stabil secara elektrostatik, sedangkan nilai potensial zeta yang lebih besar dari (+20) mV atau lebih kecil dari (-20) mV akan stabil secara sterik [14]. Nanoemulsi Astaxanthin dengan nilai potensial zeta antara (-17)-(-5) mV (mendekati 0 mV) distabilkan secara sterik oleh adanya rantai polimer surfaktan non-ionik dalam misel.…”

Section: P R O O F R E a D I N G V E R S I O Nunclassified

Formulasi dan Karakterisasi SNE (Self Nanoemulsion) Astaxanthin dari Haematococcus pluvialis sebagai Super Antioksidan Alami

2017

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ABSTRACT:Astaxanthin is a group of fat-soluble xanthophyll carotenoid found in many microorganisms and marine animals. The problem that exists in its use as active compound of antioxidants is due to lipophilicity and poor stability in the gastrointestinal tract thereby making low bioavailability. In this research offers the nanotechnology to develop astaxanthin nanoemulsion which is intended to improve the stability in the dosage form and also further developing new delivery paths in the use of antioxidants through transdermal delivery route so it has the optimal deliveries. In this research will be made nanoemulsion astaxanthin formulation to produce good physical and chemical characteristics. Nanoemulsion were prepared by using the self-nanoemulsifying (SNE) method. Optimizations of formula were performed ranging from oil phase screening, surfactant type screening, and optimization of ratio of oil phase : surfactant : co-surfactant. Characterization of nanoemulsion were carried out by physical characterizations including globul size and polydispersity index, zeta potential, visual appearance, and globul morphology. Chemical Characterization included the entrapment efficiency test. The results showed that the nanoemulsion Astaxanthin has a 10-20 nm globul size (with normal size distribution curve), the polydispersity index value is less than 0.5, the zeta potential is greater than (-20) mV, the entrapment efficiency is between 80-87%, and has spherical globules form. ABSTRAK:Astaxanthin merupakan kelompok karotenoid xantofil larut lemak yang banyak ditemukan pada berbagai mikroorganisme dan hewan laut. Permasalahan yang terdapat di dalam pengunaannya sebagai bahan aktif sumber antioksidan adalah karena lipofilisitasnya dan stabilitas astaxanthin yang rendah di dalam saluran cerna sehingga membuat ketersediaan hayati yang rendah. Di dalam penelitian ini menawarkan teknologi nano untuk mengembangkan nanoemulsi astaxanthin yang ditujukan untuk meningkatkan stabilitas astaxanthin di dalam sediaan dan juga kedepannya untuk mengembangkan jalur penghantaran baru dalam pemakaian antioksidan yakni melalui rute transdermal sehingga ditujukan agar penggunaan astaxanthin dapat optimal. Di dalam penelitian ini akan dibuat formulasi nanoemulsi astaxanthin untuk menghasilkan karakteristik fisik dan kimia yang baik. Nanoemulsi dibuat dengan menggunakan metode Nanoemulsi spontan (SNE). Dilakukan optimasi formula mulai dari skrining fase minyak, skrining jenis surfaktan, dan optimasi rasio fase minyak:surfaktan:kosurfaktan. Karakterisasi nanoemulsi berupa karakterisasi secara fisik meliputi ukuran globul dan indeks polidispersitas, potensial zeta, tampilan visual, dan morfologi globul. Karakterisasi secara kimia meliputi uji efisiensi penjeratan. Hasil penelitian menunjukkan nanoemulsi Astaxanthin yang dikembangkan memiliki ukuran globul 10-20 nm (dengan kurva distribusi ukuran globul normal), nilai indeks polidispersitas kurang dari 0.5, potensial zeta lebih besar dari (-20) mV, dan efisiensi penjeratan berkisar antara 80-87% s...

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Drug nanocrystals for the formulation of poorly soluble drugs and its application as a potential drug delivery system

Cited by 340 publications

References 53 publications

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

Nanonization of megestrol acetate by laser fragmentation in aqueous milieu

Formulasi dan Karakterisasi SNE (Self Nanoemulsion) Astaxanthin dari Haematococcus pluvialis sebagai Super Antioksidan Alami

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