Bicalutamide nanocrystals with improved oral bioavailability: <i>in vitro</i> and <i>in vivo</i> evaluation

Pokharkar, Varsha; Malhi, Tripti; Mandpe, Leenata

doi:10.3109/10837450.2012.663391

Cited by 21 publications

(11 citation statements)

References 13 publications

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“…Hence it was concluded that the crystalline nature of the drug was retained in nanoprecipitated form. This is in agreement with Hu et al (Hu et al, 2011) and Pokharkar et al (Pokharkar et al, 2013) in which nanoprecipitation of bicalutamide retained its crystalline nature. DSC DSC thermograms of pure drug ( Fig.…”

Section: Xrdsupporting

confidence: 93%

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Cardioprotective Effect of Idebenone Nanoparticles in Doxorubicin Induced Cardiomyopathy in Rats: Assessment of Myocardial Performance, Haemapoietic Parameters and Immunological Changes

Ghule¹,

Mandpe²,

Pokharkar³

et al. 2014

j pharmaceut sci pharmacol

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Doxorubicin (DXR) is an anthracycline anti-neoplastic agent associated with severe cardiotoxicity. Idebenone has recently been shown to exhibit promising results in improving cardiac performance. The objective of the present study was to develop nanoparticles of idebenone and investigate its cardioprotective effect in DXR induced cardiomyopathy. Idebenone nanoparticles were prepared by antisolvent precipitation method. Male Wistar rats were divided into three groups. The first group that underwent no treatment was accepted as control group; the second group was treated with a single intraperitoneal injection of DXR (20 mg/kg); the third group was treated with oral idebenone nanoparticles (50 mg/kg) starting 18 days before DXR injection. The blood samples were collected to measure cardiac marker enzymes CKMB and LDH, serum creatinine and oxidative stress in mononuclear cells. The architectural damage was quantified by hematoxylin eosin stain. Average mean diameter observed for idebenone nanoparticles was 0.095 ± 0.012 m. The cardiac marker enzymes were found to be elevated as compared with vehicle treated control rat. DXR treatment showed significant decrease in the activity of endogenous antioxidant enzymes and alteration in haemapoietic and immunological indices. Treatment with idebenone nanoparticles markedly improved hemodynamic and left ventricular dysfunction and reduced the levels of biological serum markers. DXR treatment also decreased cell viability and increased apoptosis in the myocardium which were prevented by the treatment with NCLI. Moreover, NCLI treatment showed anti-inflammatory and antioxidant effects as evidenced by significant increase in the activity of SOD, GPx and GST. Treatment with nanoparticles of idebenone appears to block the development of DXR mediated cardiotoxicity.

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Section: Xrdsupporting

confidence: 93%

“…Further particle surface was observed to be smoother than that of the pure drug. Thus the process of antisolvent precipitation helped in achieving desired morphology of the particles and this is in accordance with the previously published reports (Pokharkar et al, 2013;Zhang et al, 2009).…”

Section: Determination Of Saturation Solubility In Distilled Watersupporting

confidence: 90%

Cardioprotective Effect of Idebenone Nanoparticles in Doxorubicin Induced Cardiomyopathy in Rats: Assessment of Myocardial Performance, Haemapoietic Parameters and Immunological Changes

Ghule¹,

Mandpe²,

Pokharkar³

et al. 2014

j pharmaceut sci pharmacol

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“…Particle size obtained by laser diffraction is usually higher (Jacobs & Müller, 2002). Similar results were observed by Pokharkar et al (2013) where the particle size obtained by laser diffraction was 168 nm and by PCS it was 46.3 nm for bicalutamide nanosuspension prepared by antisolvent precipitation method.…”

Section: Particle Size Determinationsupporting

confidence: 86%

Engineering of polymer–surfactant nanoparticles of doxycycline hydrochloride for ocular drug delivery

Pokharkar¹,

Patil²,

Mandpe³

2014

Drug Delivery

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Context: Physiologic barriers of the eye, short precorneal drug residence time and poor corneal penetration are the few reasons for reduced ocular bioavailability. Objective: This study was aimed to develop novel polymer-surfactant nanoparticles of hydrophilic drug doxycycline hydrochloride (DXY) to improve precorneal residence time and drug penetration. Materials and methods: Nanoparticles were formulated using emulsion cross-linking method and the formulation was optimized using factorial design. The prepared formulation was characterized for particle size, potential, encapsulation efficiency, in vitro drug release and ex vivo drug diffusion studies. The antibacterial activity studies were also carried out against Escherichia coli and Staphylococcus aureus using the cup-plate method. In vivo eye irritation study was carried out by a modified Draize test in rabbits. Results and discussion: The particle size was found to be in the range of 331-850 nm. About 45-80% of the drug was found to be encapsulated in the nanoparticles. In vitro release demonstrated sustained release profile. Lower flux values in case of nanoparticles as compared to DXY pure drug solution in ex vivo diffusion studies confirmed the sustained release. The nanoparticles were found to be significantly effective (p50.001) than DXY aqueous solution due to sustained release of doxycycline from nanoparticles in both the E. coli and S. aureus strains. The formulation was found to be stable over entire stability period. Conclusion: The developed formulation is safe and suitable for sustained ocular drug delivery.

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“…To improve bioavailability and the therapeutic effectiveness of such compounds, a number of formulation strategies to increase the dissolution rate of the active and/or enhance drug solubility have been employed. For example, reducing particle size of an active ingredient has been shown to increase the rate of drug dissolution and improve bioavailability (2)(3)(4)(5). Examples of techniques to improve drug solubility include the addition of surfactants (6,7), use of co-solvents (8,9), formulating as amorphous solid dispersions (10,11), and cyclodextrin (CD) complexation (12)(13)(14)(15).…”

Section: Introductionmentioning

confidence: 99%

Experimental and Computational Studies of Physicochemical Properties Influence NSAID-Cyclodextrin Complexation

Felton

Popescu²,

Wiley

et al. 2014

AAPS PharmSciTech

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Abstract. The objective of this research was to investigate physicochemical properties of an active pharmaceutical ingredient (API) that influence cyclodextrin complexation through experimental and computational studies. Native β-cyclodextrin (B-CD) and two hydroxypropyl derivatives were first evaluated by conventional phase solubility experiments for their ability to complex four poorly watersoluble nonsteroidal anti-inflammatory drugs (NSAIDs). Differential scanning calorimetry was used to confirm complexation. Secondly, molecular modeling was used to estimate Log P and aqueous solubility (S o ) of the NSAIDs. Molecular dynamics simulations (MDS) were used to investigate the thermodynamics and geometry of drug-CD cavity docking. NSAID solubility increased linearly with increasing CD concentration for the two CD derivatives (displaying an A L profile), whereas increases in drug solubility were low and plateaued in the B-CD solutions (type B profile). The calculated Log P and S o of the NSAIDs were in good concordance with experimental values reported in the literature. Side chain substitutions on the B-CD moiety did not significantly influence complexation. Explicitly, complexation and the associated solubility increase were mainly dependent on the chemical structure of the NSAID. MDS indicated that each NSAID-CD complex had a distinct geometry. Moreover, complexing energy had a large, stabilizing, and fairly constant hydrophobic component for a given CD across the NSAIDs, while electrostatic and solvation interaction complex energies were quite variable but smaller in magnitude.

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Bicalutamide nanocrystals with improved oral bioavailability: in vitro and in vivo evaluation

Cited by 21 publications

References 13 publications

Cardioprotective Effect of Idebenone Nanoparticles in Doxorubicin Induced Cardiomyopathy in Rats: Assessment of Myocardial Performance, Haemapoietic Parameters and Immunological Changes

Cardioprotective Effect of Idebenone Nanoparticles in Doxorubicin Induced Cardiomyopathy in Rats: Assessment of Myocardial Performance, Haemapoietic Parameters and Immunological Changes

Engineering of polymer–surfactant nanoparticles of doxycycline hydrochloride for ocular drug delivery

Experimental and Computational Studies of Physicochemical Properties Influence NSAID-Cyclodextrin Complexation

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