Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

S, Kalvakuntla; Deshpande, Mangesh C.; Attari, Zenab; Kunnatur, B K

doi:10.15171/apb.2016.013

Cited by 36 publications

(32 citation statements)

References 17 publications

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“…Thus SEM pictures confirmed that the larger scaly particles of EE were successfully converted to nearly elongated, smaller sized nanoparticles with a smoother surface on size reduction. The particle size of EENS increased after lyophilization but were still smaller than that of EE [33] .…”

Section: Resultsmentioning

confidence: 91%

“…SEM studies were performed using an SEM (Jeol JSM-6360, Japan) at 20 kV accelerating voltage and high vacuum. Before analysis, lyophilized EENS were first placed on two-sided carbon tape and then, sputtered with gold-palladium alloy up to 3-5 nm of thickness [30,33] .…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

“…Samples (5 ml each) were withdrawn at 10, 20, 30, 40, 50 and 60 min time intervals and the fresh buffer was added to maintain the sink conditions. The samples were collected and filtered using Whatman filter paper (0.25 µm, Whatman Inc., USA) and analyzed using UV spectrophotometer at 280 nm [33,34] .…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

“…As a stabilizer moreover, soya lecithin has a thick coat on the surface of EENS which played a vital role in bioavailability enhancement. It is an amphiphilic surfactant, that enhanced EE penetration ability and thus promoted rapid permeation of the EE nanoparticles through the intestinal epithelium and finally into the systemic circulation [33] .…”

Section: Fig 5: Cytotoxicity Of Eens and Eeaqd Cytotoxicity Of Ethinmentioning

confidence: 99%

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Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Powar¹,

Hajare²

2020

ijps

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The present investigation was aimed to fabricate lyophilized nanosuspension of poorly soluble ethinylestradiol in order to enhance oral bioavailability and stability. The top-down high-pressure homogenization technique was used to formulate the desired dosage form. The formulations were characterized and optimized for compatibility, crystallographic investigation, surface topography, drug release, in vitro apoptosis and cytotoxicity and in vivo pharmacokinetic investigations. The mean particle size and zeta potential of the optimized lyophilized ethinylestradiol nanosuspension were 220±0.37 nm and -19.3±6.73 mV, respectively. The surface topographical studies showed needle-shaped particles from bar shape upon nanonization by high-pressure homogenization technique. Differential scanning calorimetry and X-ray powder diffraction studies confirmed the crystalline nature of ethynylestradiol after nanonization. The dissolution rate of ethinylestradiol nanosuspension was improved as compared to ethinylestradiol powder. In vitro cytotoxicity of ethinylestradiol nanosuspension on MCF-7 cell line showed more than 80 % inhibition of viability of cells relative to that produced by ethinylestradiol aqueous dispersion. Noteworthy, apoptotic cells treated with ethinylestradiol nanosuspension showed shrinkage, followed by fragmentation and cell death. Significantly, ethinylestradiol nanosuspension enhanced C max and AUC 0-t by 1.5-fold and 1.7-fold compared to that of the aqueous solution. The relative bioavailability of ethinylestradiol was enhanced 2-fold and high concentrations were found to be distributed to liver, spleen and stomach. Thus lyophilized nanosuspension could be a better approach to enhance solubility, oral bioavailability and stability of ethinylestradiol in pharmaceutical formulations.

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Section: Resultsmentioning

confidence: 91%

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Section: In Vitro Dissolution Studymentioning

confidence: 99%

Section: Fig 5: Cytotoxicity Of Eens and Eeaqd Cytotoxicity Of Ethinmentioning

confidence: 99%

See 2 more Smart Citations

Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Powar¹,

Hajare²

2020

ijps

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show abstract

“…10 mL portion of the freshly prepared and cooled nanosuspension was centrifuged at 1000 rpm for 10 minute using a Remi centrifuge. The supernatant was removed and the amount of unincorporated drug was measured by taking the absorbance of the supernatant solution at 289 nm by using UV spectrophotometer [18].…”

Section: Entrapment Efficiencymentioning

confidence: 99%

Formulation optimization and evaluation of Cefdinir nanosuspension using 23 Factorial design

Patil¹,

Patil²,

Mane³

et al. 2018

jrp

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Poor water solubility and slow dissolution rate are the prime issues for the majority of upcoming and existing biologically active compounds. Cefdinir is a poorly water-soluble drug and its bioavailability is very low from its crystalline form. The purpose of the present investigation was to increase the solubility and dissolution rate of Cefdinir by preparation of its nanosuspension by solvent evaporation technique. The prepared formulation of nanosuspension was evaluated for its particle size, total drug content, entrapment efficiency, saturation solubility and in vitro dissolution. The optimized formulation was spray dried to obtain nanoparticles. The prepared nanoparticles were then evaluated for their particle size, saturation solubility and in-vitro drug release and the results were compared with the pure drug. A 2 3 factorial design was employed to study the effect of independent variables, amount of PVPK-30 (X1), Poloxamer-188 (X2) and stirring rate (X3) on the dependent variables, particle size (nm,Y1) and in-vitro drug release (%, Y2). Validity of the developed mathematical equation was assayed by designing to check point. The results indicated the suitability of solvent evaporation method for Cefdinir with improved in vitro dissolution rate and thus perhaps enhance fast onset of action for the drug.

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Challenges in the Development of Intravenous Neurokinin‐1 Receptor Antagonists: Results of a Safety and Pharmacokinetics Dose‐Finding, Phase 1 Study of Intravenous Fosnetupitant

Tyler

Schultz

Venturini

et al. 2022

Clinical Pharm in Drug Dev

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Oral NEPA is the fixed‐combination antiemetic comprising netupitant (neurokinin‐1 receptor antagonist [NK1RA]) and palonosetron (5‐hydroxytryptamine‐3 receptor antagonist [5‐HT3 RA]). Intravenous (IV) NEPA, containing fosnetupitant, a water‐soluble N‐phosphoryloxymethyl prodrug of netupitant, has been developed. Fosnetupitant does not require excipients or solubility enhancers often used to increase IV NK1RA water solubility, preventing the occurrence of hypersensitivity and infusion‐site reactions associated with these products. In this phase 1 study, subjects received a 30‐minute placebo or fosnetupitant (17.6–353 mg) infusion and an oral NEPA or placebo capsule, with 2‐sequence crossover treatment for fosnetupitant 118‐ to 353‐mg dose cohorts. IV fosnetupitant safety and pharmacokinetics were evaluated, and its equivalence to an oral netupitant 300‐mg dose was defined. Overall, 158 healthy volunteers were enrolled. All adverse events (AEs) were mild or moderate in intensity. Doppler‐identified infusion‐site asymptomatic thrombosis occurred in 5.4% (fosnetupitant) and 1.2% (oral NEPA) of subjects. The frequency or number of treatment‐related AEs did not increase with ascending fosnetupitant doses. The most common treatment‐related AEs were headache (fosnetupitant, 8.1%; oral NEPA, 12.7%) and constipation (fosnetupitant, 1.4%; oral NEPA, 7.5%). A fosnetupitant 235‐mg dose was equivalent, in terms of netupitant exposure, to 300‐mg oral netupitant. The safety profile of a single fosnetupitant 235‐mg infusion was similar to that of single‐dose oral NEPA.

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Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

Cited by 36 publications

References 17 publications

Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Formulation optimization and evaluation of Cefdinir nanosuspension using 23 Factorial design

Challenges in the Development of Intravenous Neurokinin‐1 Receptor Antagonists: Results of a Safety and Pharmacokinetics Dose‐Finding, Phase 1 Study of Intravenous Fosnetupitant

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