Nanosuspension Technologies for Delivery of Poorly Soluble Drugs

Yadollahi, Roya; Vasilev, Krasimir; Simović, Spomenka

doi:10.1155/2015/216375

Cited by 88 publications

(52 citation statements)

References 124 publications

(113 reference statements)

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“…One approach to producing nanosuspensions is using the top-down technique, in which the large drug particles are broken down into smaller ones (i.e., nanosuspensions) by using high-pressure homogenisation (HPH). The resultant nanosuspensions are of a nanometre size and have a high surface area to volume ratio [9]. The nanoparticles are stabilized in an aqueous medium using stabilizer that are generally recognized as safe [10].…”

Section: Introductionmentioning

confidence: 99%

Development and In Vitro Evaluation of a Zerumbone Loaded Nanosuspension Drug Delivery System

Kit

Jagdish

et al. 2018

Crystals

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Zerumbone extracted from the volatile oil of rhizomes available from the Zinigiber zerumbet has promising pharmacological activity. However, it has poor aqueous solubility and dissolution characteristics. To improve this, a nanosuspension formulation of zerumbone was developed. Nanosuspensions were formulated using high-pressure homogenization (HPH) with sodium dodecyl sulphate (SDS) and hydroxypropylmethylcellulose (HPMC) as stabilizers; the formulation was optimized and freeze dried. The optimized nanosuspension product was evaluated using an optical light microscope, photon correlation spectroscopy (PCS), polydispersity index, zeta potential, SEM, differential scanning calorimetry (DSC) and FT-IR. The physical stability of the nanosuspensions was evaluated for 30 days at 4 • C, 25 • C, and 37 • C. To validate the theoretical benefit of the increased surface area, we determined an in vitro saturation solubility and dissolution profile. The mean particle size, polydispersity index and zeta potential of the zerumbone nanosuspensions stabilized by SDS versus HPMC were found to be 211 ± 27 nm vs. 398 ± 3.5 nm, 0.39 ± 0.06 vs. 0.55 ± 0.004, and −30.86 ± 2.3 mV vs. −3.37 ± 0.002 mV, respectively. The in vitro saturation solubility and dissolution revealed improved solubility for the zerumbone nanosuspension. These results suggested that the nanosuspensionlization improves the saturation solubility and dissolution profile of zerumbone, which may facilitate its use as a therapeutic agent in the future.

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Section: Introductionmentioning

confidence: 99%

Development and In Vitro Evaluation of a Zerumbone Loaded Nanosuspension Drug Delivery System

Kit

Jagdish

et al. 2018

Crystals

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“…The proportion of poorly water‐soluble compounds among drug candidates in the discovery stage has increased over the past decade (Lipinski, , ). Recently, nanosuspension technologies have been developed to increase the bioavailability of poorly water‐soluble drugs (Gao et al ., ; Liversidge et al ., ; Müller et al ., ; Sutradhar et al ., ; Müller & Peters, ; Neervannan, ; Yadollahi et al , ). In a previous study, we optimized a preparation method of nanosuspensions for oral administration using a rotation/revolution mixer and confirmed its enhancing effect on exposure in rats (Komasaka et al ., ).…”

Section: Introductionmentioning

confidence: 99%

Nanosuspension formulations of poorly water‐soluble compounds for intravenous administration in exploratory toxicity studies: in vitro and in vivo evaluation

Fujimura¹,

Komasaka

Tomari³

et al. 2016

J of Applied Toxicology

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This study was conducted to investigate the use of a nanosuspension for intravenous injection into dogs to increase exposure without toxic additives for preclinical studies in the discovery stage. Nanosuspensions were prepared with a mixer mill and zirconia beads with a vehicle of 2% (w/v) poloxamer 338, which was confirmed to lead to no histamine release in dogs. Sterilized nanosuspensions of poorly water-soluble compounds, cilostazol (Cil), spironolactone (Spi) and probucol (Pro), at 10 mg ml À1 were obtained by milling for 30 min, followed by autoclaving for 20 min at 121°C and milling for 30 min (mill-autoclave-mill method). The particle sizes (d50) of Cil, Spi and Pro were 0.554, 0.484 and 0.377 μm, respectively, and the percentages of the nominal concentration were 79.1%, 99.6% and 75.4%, respectively. In chromatographic data, no extra peaks were observed. The particle size of Cil was 0.564 μm after storage for 16 days at 2-8°C. Cil in nanosuspension, but not in microsuspension, rapidly dissolved in dog plasma. Cil nanosuspension at 0.4 mg kg À1 and Cil saline solution at 0.03 mg kg À1 , around the saturation solubility, were intravenously administered to dogs. Nanosuspension increased exposure. The versatility of the mill-autoclave-mill method was checked for 15 compounds, and the particle size of 12 compounds was in the nano range. The nanosuspension optimized in this study may be useful for intravenous toxicological and pharmacological studies in the early stage of drug development.

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“…Nano suspensions consist of poorly water soluble drugs size below 1µm with or without any matrix material, 16 which are stabilized by surfactants and polymers. 17 In the present study various meropenem nanosuspensions were prepared by emulsification solvent evaporation technique. The formed nano formulations were almost spherical and uniform in size.…”

Section: Resultsmentioning

confidence: 99%

Solubility and Dissolution Enhancement of Meropenem by Nano Suspension Approach

chirumamilla¹,

Padasala²,

Aravally³

et al. 2017

JYP

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Objective: To prepare and evaluate the suitable nanosuspensions of Meropenem (BCS-IV drug) to increase its solubility and dissolution. Methodology: The meropenem nanosuspensions were prepared by emulsification solvent evaporation technique by applying ultrasonic energy through probe sonicator, where the organic phase of drug solution in methanol was emulsified in aqueous phase containing hydroxy propyl methyl cellulose as solubilizer and sodium lauryl sulphate as stabilizer. The prepared nanosuspensions were characterised for particle size, zeta potential, surface morphology by SEM, drug excipient compatibility by FTIR and DSC and conducted in-vitro drug release studies. Results: Results showed that the prepared nanosuspensions were having particle size range from 1 to 1000nm and the zeta potential from -10 to -20 mVs. Scanning electron microscopic pictures revealed that the obtained nanosuspension particles were spherical in shape with surface smoothness and in-vitro drug release studies notified that the prepared nanosuspensions showed increase in solubility and dissolution of meropenem when compared with the pure form. Conclusion: The nanosuspensions of meropenem could be successfully prepared and can be concluded that the nanosuspension formulation is a promising approach to increase the solubility and dissolution of BCS-IV drugs like meropenem.

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Nanosuspension Technologies for Delivery of Poorly Soluble Drugs

Cited by 88 publications

References 124 publications

Development and In Vitro Evaluation of a Zerumbone Loaded Nanosuspension Drug Delivery System

Development and In Vitro Evaluation of a Zerumbone Loaded Nanosuspension Drug Delivery System

Nanosuspension formulations of poorly water‐soluble compounds for intravenous administration in exploratory toxicity studies: in vitro and in vivo evaluation

Solubility and Dissolution Enhancement of Meropenem by Nano Suspension Approach

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