Oral formulation strategies to improve solubility of poorly water-soluble drugs

Singh, Abhishek; Worku, Zelalem Ayenew; Mooter, Guy Van den

doi:10.1517/17425247.2011.606808

Cited by 205 publications

(96 citation statements)

References 84 publications

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“…Currently, complexes with cyclodextrins are used in pharmaceutical industry to increase the solubility and bioavailability of drugs 52 . Cyclodextrins are cyclic oligosaccharides with a hydrophilic outer surface and a lipophilic central cavity.…”

Section: Calculationmentioning

confidence: 99%

Synthesis, antimicrobial and anticonvulsant screening of small library of tetrahydro-2H-thiopyran-4-yl based thiazoles and selenazoles

Łączkowski

Biernasiuk

Baranowska-Łączkowska

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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Synthesis and investigation of antimicrobial activity of 22 novel thiazoles and selenazoles derived from dihydro-2H-thiopyran-4(3H)-one are presented. Additionally, anticonvulsant activity of six derivatives is examinated. Among the derivatives, compounds 4a-f, 4i, 4k, 4 l, 4n, 4o-s and 4v have very strong activity against Candida spp. with MIC ¼ 1.95-15.62 mg/ml. In the case of compounds 4a-f, 4i, 4k, 4 l, 4n, 4o, 4r and 4s, the activity is very strong against some strains of Candida spp. isolated from clinical materials, with MIC ¼ 0.98 to 15.62 mg/ml. Additionally, compounds 4n-v are found to be active against Gram-positive bacteria with MIC ¼ 7.81-62.5 mg/ml. The results of anticonvulsant screening reveal that compounds 4a, 4b, 4m and 4n demonstrate a statistically significant anticonvulsant activity in the pentylenetetrazole model, whereas compounds 4a and 4n showed protection in 6-Hz psychomotor seizure model. Noteworthy, none of these compounds impaired animals' motor skills in the rotarod test. We also performed quantum chemical calculation of interaction and binding energies in complex of 4a with cyclodextrin.

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Section: Calculationmentioning

confidence: 99%

Synthesis, antimicrobial and anticonvulsant screening of small library of tetrahydro-2H-thiopyran-4-yl based thiazoles and selenazoles

Łączkowski

Biernasiuk

Baranowska-Łączkowska

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…(Singh et al, 2011). The use of mesoporous silica is one of the more rapidly developing formulation techniques for enhancing the solubility of poorly water-soluble drugs (Vialpando et al, 2011;Mamaeva et al, 2013;Santos et al, 2013;Shen et al, 2013;Xu et al, 2013;Wang et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

Improving anti-tumor activity of sorafenib tosylate by lipid- and polymer-coated nanomatrix

et al. 2017

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In the present study, we select the Sylysia 350 (Sylysia) as mesoporous material, distearoylphosphatidylethanolamine-poly(ethylene glycol) 2000 (DSPE-PEG) as absorption enhancer and hydroxy propyl methyl cellulose (HPMC) as crystallization inhibitor to prepare sorafenib tosylate (SFN) nanomitrix (MSNM@SFN) for improving the anti-tumor activity of SFN. The MSNM@SFN was prepared by solvent evaporation method. The solubility, dissolution, and bioavailability of SFN in MSNM@SFN were also investigated. The anti-tumor activity of MSNM@SFN was evaluated in vitro and in vivo. Our results indicated that the solubility and dissolution of SFN in MSNM@SFN were significantly increased. The oral bioavailability of SFN in MSNM@SFN was greatly improved 7.7-fold compared with that in SFN suspension. The enhanced anti-tumor activity of MSNM@SFN was confirmed in vitro and in vivo experiments. This nanomatrix developed in this study could be a promising drug delivery platform for improving the therapeutic efficacy of poorly water-soluble drugs.

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“…Nanosizing of drug particles has been proven to be a tangible option for achieving enhanced solubility [33]. Formulating drugs with water soluble polymers, surfactants, lipids and other excipient can also lead to enhanced solubility [34,35]. EASAI method is an effective method for the preparation of both bare drug nanoparticles as well as polymer stabilized nanoparticles with average particle size well below 100 nm.…”

Section: Introductionmentioning

confidence: 99%

Unusual anti-leukemia activity of nanoformulated naproxen and other non-steroidal anti-inflammatory drugs

Kumar

Siril

Javid

2016

Materials Science and Engineering: C

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The non-steroidal anti-inflammatory drugs (NSAIDs) are the most widely used pharmaceuticals worldwide. Interestingly, many of them have significant anticancer properties too. However, the poor water solubility of certain NSAIDs limits their application for cancer treatment. Nanosizing of such drugs can help to improve the solubility and this may result in enhanced anticancer activities too. Moreover, over dosages and the accompanying side effects of NSAIDs can be minimized by improving their solubility and bioavailability. Successful nanoformulation of three NSAIDs: ibuprofen (IBP), ketoprufen (KP) and naproxen (NAP) using a novel evaporation assisted solvent-antisolvent interaction (EASAI) method is reported here. Three water soluble and biocompatible polymers: polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA) and hydroxypropyl methylcellulose (HPMC) were used to stabilize the drug nanoparticles. Particles having spherical morphology with average size below 30 nm were thoroughly characterized using dynamic light scattering and field emission scanning electron microscopy (FESEM) imaging. The nanoformulation resulted in ten to fifteen fold improvements in the solubility and significant enhancement in the in-vitro drug release profiles of the NSAIDs. Anticancer screening of the nanoformulated NSAIDs against five different cancer cell lines such as MCF-7 (Human breast cancer cell line), (Human pancreatic cancer cell line) MIA-PA-CA-2, (Human colon cancer cell line) HT-29, (Human leukemia cell line) Jurkat and (human ovarian carcinoma cell line) A2780 was performed. All the nanoformulated samples showed improved anticancer activity against the Leukemia cancer cell line, out of which NAP-PVP showed the highest anti-cancer activity. The anti-Leukemia activity of NAP-PVP was more than twice that of doxorubicin which is a standard anticancer drug.

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Oral formulation strategies to improve solubility of poorly water-soluble drugs

Cited by 205 publications

References 84 publications

Synthesis, antimicrobial and anticonvulsant screening of small library of tetrahydro-2H-thiopyran-4-yl based thiazoles and selenazoles

Synthesis, antimicrobial and anticonvulsant screening of small library of tetrahydro-2H-thiopyran-4-yl based thiazoles and selenazoles

Improving anti-tumor activity of sorafenib tosylate by lipid- and polymer-coated nanomatrix

Unusual anti-leukemia activity of nanoformulated naproxen and other non-steroidal anti-inflammatory drugs

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