Qualitative and quantitative evaluation of prostatic histomorphology in rats following chronic treatment with finasteride, a 5-alpha reductase inhibitor

Prahalada, S.; Keenan, Kevin P.; Hertzog, Phillip R.; Gordon, Lea R.; Peter, C. P.; Soper, Keith A.; Zwieten, Matthew J. van; Bokelman, Delwin L.

doi:10.1016/0090-4295(94)90184-8

Cited by 33 publications

(19 citation statements)

References 18 publications

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“…15 An increase in the level of DHT in the prostate results in prostate hyperplasia and urinary tract obstruction. 16 The drug is practically insoluble in water, with a mean bioavailability of 63%.…”

Section: Introductionmentioning

confidence: 99%

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Ahmed¹

2016

IJN

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In this study, optimized freeze-dried finasteride nanoparticles (NPs) were prepared from drug nanosuspension formulation that was developed using the bottom–up technique. The effects of four formulation and processing variables that affect the particle size and solubility enhancement of the NPs were explored using the response surface optimization design. The optimized formulation was morphologically characterized using transmission electron microscopy (TEM). Physicochemical interaction among the studied components was investigated. Crystalline change was investigated using X-ray powder diffraction (XRPD). Crystal growth of the freeze-dried NPs was compared to the corresponding aqueous drug nanosuspension. Freeze-dried NPs formulation was subsequently loaded into hard gelatin capsules that were examined for in vitro dissolution and pharmacokinetic behavior. Results revealed that in most of the studied variables, some of the quadratic and interaction effects had a significant effect on the studied responses. TEM image illustrated homogeneity and shape of the prepared NPs. No interaction among components was noticed. XRPD confirmed crystalline state change in the optimized NPs. An enhancement in the dissolution rate of more than 2.5 times from capsules filled with optimum drug NPs, when compared to capsules filled with pure drug, was obtained. Crystal growth, due to Ostwald ripening phenomenon and positive Gibbs free energy, was reduced following lyophilization of the nanosuspension formulation. Pharmacokinetic parameters from drug NPs were superior to that of pure drug and drug microparticles. In conclusion, freeze-dried NPs based on drug nanosuspension formulation is a successful technique in enhancing stability, solubility, and in vitro dissolution of poorly water-soluble drugs with possible impact on the drug bioavailability.

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Section: Introductionmentioning

confidence: 99%

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Ahmed¹

2016

IJN

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“…It is well known that administration of finasteride to dogs induces a sustained, dose-dependent atrophy of the glandular and fibro-muscular compartments of the prostate [21]. The shrinkage of the prostate, therefore, results from an effect on all prostatic compartments and not only on the epithelium.…”

Section: Discussionmentioning

confidence: 99%

Immunohistochemical Studies of the Effect of Chlormadinone Acetate (CMA) on Prostatic Hyperplasia.

Murakoshi

Ikeda

Tagawa

et al. 2002

Acta Histochem. Cytochem

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“…Studies in rats with high dose finasteride showed atrophy of the prostate gland of animals [10][11][12] , and there is evidence that the prostatic glandular atrophy with finasteride is secondary to blockage of apoptosis promoted by 5áR…”

Section: Discussion Discussion Discussion Discussion Discussionmentioning

confidence: 99%

O impacto na expressão agnors e apoptose na próstata do hamster-mesocricetus auratus (HMA) submetido à aplicação de finasterida

Vidigal¹,

Silva²,

Vidigal³

2011

Rev. Col. Bras. Cir.

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ABSTRACT ABSTRACT ABSTRACTObjective Objective Objective Objective Objective: To evaluate the impact on the AgNORs expression and apoptosis in the prostate of the hamster-Mesocricetus auratus (HMA) submitted to the application of finasteride. Methods Methods Methods Methods Methods: Twenty male rodents of the species HMA (n = 20) were randomly assigned to groups of ten animals: Finasteride group (n = 10) and the Control group (n = 10). In the finasteride group 7.14 ng / mL finasteride was subcutaneously (SC) administered on the back of the animals three times a week for 90 days. AgNOR expression was evaluated as a marker of cell proliferation and apoptosis as a marker of cell death. Results Results ResultsResults Results: The expression of AgNORs was lower in the finasteride group, 2.846 ± 0.877 vs. 3.68 ± 1.07 argyrophilic regions per square micrometer (µm2) in the control group, p = <0.0001. Apoptosis was more frequent in the finasteride group, 53.62 ± 1.389 versus 14.76 ± 2.13 per µm2 in the control group, p = 0. . Investigations in animals with markers of proliferation and cell death may be of interest to corroborate these results.The anatomy, histology and physiology of the prostate of the hamster -Mesocricetus auratus (HMA) -were described by Toma et al. 5, allowing the realization of experiments with these animals with medications that can act in this gland.Vidigal et al. 6 studied the prostates of the HMA, when they had the opportunity to know the anatomy and histology of this gland. Combining theory with practice, they realized that these rodents were suitable for the development of research as experimental animals.The objective of this study therefore is to assess the impact on AgNOR expression (Argyrophilic Nuclear Organizer Regions), a marker of cell proliferation, apoptosis and cell death in the prostate of HMA submitted to finasteride treatment. We studied 20 adult HMA rodents randomly selected from those available in a vivarium, aged one year, divided into two groups: finasteride group, consisting of ten animals (n = 10); and control group, also formed by ten animals (n = 10). METHODS METHODS METHODS METHODS METHODS Experimental designThe hamsters were purchased from the animal house of the Institute of Biological Sciences, Federal University of Minas Gerais (ICB-UFMG), Belo Horizonte, Minas Gerais, Brazil. The finasteride group weighed 145 ± 15.27 g, and control group 129 ± 18.82 g.The animals were housed in plastic cages measuring 40cmx60cmx20cm (two animals per unit) and lined with wood shavings. They were fed ad libitum with chow prepared for hamsters and sunflower seeds, peanuts Vidigal Vidigal Vidigal Vidigal Vidigal The impact in the agnors expression and apoptosis in the prostate of hamster-mesocricetus auratus (HMA) submitted to finasteride application 335 Rev. Col. Bras. Cir. 2011; 38(5): 334-337 and corn. Water was offered to the animals in suction fountains. They were exposed to indirect light from 6 am to 18h and darkness for twelve hours at a temperature of 21° C.The...

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Qualitative and quantitative evaluation of prostatic histomorphology in rats following chronic treatment with finasteride, a 5-alpha reductase inhibitor

Cited by 33 publications

References 18 publications

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Immunohistochemical Studies of the Effect of Chlormadinone Acetate (CMA) on Prostatic Hyperplasia.

O impacto na expressão agnors e apoptose na próstata do hamster-mesocricetus auratus (HMA) submetido à aplicação de finasterida

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