Liquid antisolvent precipitation and stabilization of nanoparticles of poorly water soluble drugs in aqueous suspensions: Recent developments and future perspective

Thorat, Alpana A.; Dalvi, Sameer V.

doi:10.1016/j.cej.2011.12.044

Cited by 347 publications

(239 citation statements)

References 215 publications

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“…The stirring device is one of the factors that affects mixing efficiency. 32 For this purpose, various mixing/stirring devices (namely, magnetic stirrer, rotor stator homogenizer, over-head stirrer, and sonicator bath) were compared depending on both the particle size and PdI of the RIF NS. As shown in Table 2, the four mixing devices achieved a particle size within a range of 173-353 nm with PdI ranging from 0.215 to 0.456.…”

Section: Selection Of the Stirring Methodsmentioning

confidence: 99%

“…34 The possible mechanism of polymer adsorption on the crystal surface may be by either formation of hydrogen bonds between the drug molecules and the polymer or the incorporation of drug molecules into crystal lattice. 32 Thus, 0.4% w/v PVA was chosen as an optimum stabilizer concentration for further investigation.…”

Section: Effect Of the Stabilizer Concentrationmentioning

confidence: 99%

“…Several reports showed that Ostwald ripening and particle growth were the consequences of residual organic solvents. 32,33 Therefore, methanol was chosen as a RIF suitable solvent for NS preparation.…”

Section: Process Variables Of the Nanoprecipitation Technique Selectimentioning

confidence: 99%

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The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

Mohyeldin

Mehanna

Elgindy

2016

IJN

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Purpose This article investigated the influence of novel rifampicin nanosuspension (RIF NS) for enhancing drug delivery properties. Methods RIF NS was fabricated using the antisolvent precipitation technique. The impact of solvent type and flow rate, stabilizer type and concentration, and stirring time and apparatus together with the solvent–antisolvent volume ratio on its controlled nanocrystallization has been evaluated. NSs were characterized by transmission electron microscopy, particle size and zeta potential analysis, solubility, and dissolution profiles. The compatibility between RIF and the stabilizer was investigated via Fourier transform infrared spectroscopy and the differential scanning calorimetry techniques. The shelf-life stability of the RIF NS was assessed within a period of 3 months at different storage temperatures. Cell cytotoxicity was evaluated using 3(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on lung epithelial cells. Results Polyvinyl alcohol at 0.4% w/v, 1:15 methanol to deionized water volume ratio and 30-minutes sonication were the optimal parameters for RIF NS preparation. Nanocrystals were obtained with a nanometeric particle size (101 nm) and a negative zeta potential (−26 mV). NS exhibited a 50-fold enhancement in RIF solubility and 97% of RIF was dissolved after 10 minutes. The RIF NS was stable at 4±0.5°C with no significant change in particle size or zeta potential. The MTT cytotoxicity assay of RIF NS demonstrated a good safety profile and reduction in cell cytotoxicity with half maximal inhibitory concentration values of 0.5 and 0.8 mg/mL for free RIF and RIF NS, respectively. Conclusion A novel RIF NS could be followed as an approach for enhancing RIF physicochemical characteristics with a prominence of a safer and better drug delivery.

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Section: Selection Of the Stirring Methodsmentioning

confidence: 99%

Section: Effect Of the Stabilizer Concentrationmentioning

confidence: 99%

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The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

Mohyeldin

Mehanna

Elgindy

2016

IJN

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“…28) In addition, the polar nature of the polyphenols is drawback for a delivery through the skin barrier, and 29) consisting of HMHEC and lecithin 30) of more than 95%, 31) was therefore prepared in this present study as a delivery system in a comparison with a commercial liposome ( Table 4). The content of cellulose polymer was increased to improve steric stabilization, providing more surface coverage area and higher excluded volume limiting the nucleation process of the liposome, 32) and loaded with 50 mg/mL the Salak plum peel EtOAc fraction. The mild acid Salak plum peel liposome, which in the range of 5.5-7 indicates stable formulation acceptably used in cosmetics, 33) was HMHEC-dependent, but the pH of the commercial liposome was lowest and out of the safety range of topical formulation.…”

Section: Preparation and Stability Of The Salak Plum Peel Etoac Fractmentioning

confidence: 99%

Salak Plum Peel Extract as a Safe and Efficient Antioxidant Appraisal for Cosmetics

Kanlayavattanakul¹,

Lourith²,

Ospondpant³

et al. 2013

Bioscience, Biotechnology, and Biochemistry

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The antioxidant activities of Salak plum (Salacca edulis) peel extracts were assessed by 1, 1-diphenyl-2-picrylhydrazyl (DPPH), 2,2 0 -azino-bis(3-ethylbenzothaiazoline)-6-sulfonic acid (ABTS), and ferric reducing ability of plasma (FRAP) assays. The ethyl acetate (EtOAc) fraction was the most potent (DPPH IC50 ¼ 2:932 AE 0:030 g/mL, ABTS IC50 ¼ 7:933 AE 0:049 g/mL, FRAP EC ¼ 7;844:44 AE 40:734). Chlorogenic acid was detected as the marker (1:400 AE 0:102 g/kg). The EtOAc fraction was non-cytotoxic in vero and normal human fibroblast (NHF) cells. It exhibited cellular oxidative prevention and damage treatment at 5-40 g/mL in NHF cells. Salak plum peel loaded liposome consisting of lecithin and hydrophobically modified hydroxyethylcellulose (HMHEC) was developed and found stable with adequate entrapment efficacy. Thus Salak plum peel was highlighted as a potential ecological antioxidant for health promotion aspects, and for cosmetics.

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“…These classes have the limited bioavailability of drugs due to their low solubility and dissolution rate [1]. The bioavailability is defined as the percentage of the quantity of the drug absorbed compared to its initial quantity of dosage, which can be improved by a decrease in their particle size [2].…”

Section: Introductionmentioning

confidence: 99%

Antisolvent Crystallization of Poorly Water Soluble Drugs

Lonare¹,

Patel²

2013

IJCEA

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Abstract-The enhancement in bioavailability of the drugs is one of the most important concerning aspects of the pharmaceutical industries. Preparation of nanoparticles or microparticles of these drugs is the newest formulation strategies. The size and morphology of a drug are affecting several essential pharmaceutical properties. In general, the drug delivery system needs narrow particle size distribution with regular particle shape, particularly, an engineered drug particles to meet biopharmaceutical and processing needs. An antisolvent crystallization technique is being used to prepare nanoparticles or microparticles for poorly water soluble drugs at research scale. This method has an ability to change the solid-state properties of pharmaceutical substances including the modification of crystal formation and particle size distributions. Therefore, various operating variables and their effect on the particle size of poorly water soluble drugs in an anti-solvent crystallization have been reviewed.

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Liquid antisolvent precipitation and stabilization of nanoparticles of poorly water soluble drugs in aqueous suspensions: Recent developments and future perspective

Cited by 347 publications

References 215 publications

The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

The relevancy of controlled nanocrystallization on rifampicin characteristics and cytotoxicity

Salak Plum Peel Extract as a Safe and Efficient Antioxidant Appraisal for Cosmetics

Antisolvent Crystallization of Poorly Water Soluble Drugs

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