Topical Formulations Containing Finasteride. Part I: In Vitro Permeation/Penetration Study and In Vivo Pharmacokinetics in Hairless Rat

Monti, Daniela; Tampucci, Silvia; Burgalassi, Susi; Chetoni, Patrizia; Lenzi, Carla; Pirone, Andrea; Mailland, F.

doi:10.1002/jps.24028

Cited by 26 publications

(18 citation statements)

References 47 publications

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“…The 4‐fold increase in epidermis retention obtained with P‐10–008, notwithstanding quantitatively lower than that obtained with P‐08–016, may be indicative of an effect of the formulation on the interfollicular pathway that could lead over time to a higher skin permeation as previously observed …”

Section: Resultssupporting

confidence: 52%

“…The 4-fold increase in epidermis retention obtained with P-10-008, notwithstanding quantitatively lower than that obtained with P-08-016, may be indicative of an effect of the formulation on the interfollicular pathway that could lead over time to a higher skin permeation as previously observed. 28 Probably, the high amounts of propylene glycol and ethanol in formulation P-10-008 require longer time to affect the barrier properties of SC, opening ways for the passage of drugs. 37 As far as the aim of our work was to target the pilosebaceous unit as depot of FNS for localized therapy without systemic effects, formulation P-08-016 seems to reach the goal.…”

Section: Skin Deposition Studiesmentioning

confidence: 99%

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Topical Formulations Containing Finasteride. Part II: Determination of Finasteride Penetration into Hair Follicles using the Differential Stripping Technique

Tampucci

Burgalassi

Chetoni

et al. 2014

Journal of Pharmaceutical Sciences

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Section: Resultssupporting

confidence: 52%

Section: Skin Deposition Studiesmentioning

confidence: 99%

Topical Formulations Containing Finasteride. Part II: Determination of Finasteride Penetration into Hair Follicles using the Differential Stripping Technique

Tampucci

Burgalassi

Chetoni

et al. 2014

Journal of Pharmaceutical Sciences

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“…Linear regression analysis of pseudo steady-state diffusion data allowed calculation of J, the steady-state flux (given by Q/A•t, where Q is the amount of permeant diffusing across the area A in time t) normalized to the thickness of the biological substrate and amount of drug permeated NYST In Vitro Release Through Cellulose Acetate Membranes In vitro release of NYST from the V1-G1-G1/Et formulations through cellulose acetate membranes (SpectraPore3, MWCO3500, Spectrum®, NL) was investigated using vertical Gummer cells ( 22 ) with an effective diffusion area of 1.23 cm . Five milliliters of 25 mM HEPES buffer (pH 7.4) plus 154 mM NaCl, thermostated at 32°C and stirred at 600 rpm, were used as the receptor medium.…”

Section: Nyst Delivery/permeation Experimentsmentioning

confidence: 99%

Influence of a Combination of Chemical Enhancers and Iontophoresis on In Vitro Transungual Permeation of Nystatin

et al. 2018

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To promote transungual permeation of nystatin (NYST), molecule with high molecular weight, no water-soluble, amphoteric by iontophoresis. The synergic effect of the combination of cetylpyridinium chloride, CPC, or polyoxyethylene (20) sorbitan monooleate, TW80, and iontophoresis was investigated. In vitro permeation experiments were carried out through bovine hoof slices using vertical diffusion cells. A low current density (0.2 mA/cm) was applied by introducing Ag/AgCl electrodes in the donor (anode) and receptor (cathode) chambers. The donor phase consisted of a solution, a suspension, or gel-type vehicles containing NYST and surfactants in pH 5.6 HEPES buffer. The addition of CPC to NYST suspension (SOSP) produced a fivefold increase on the permeability of the bovine hoof membrane to the drug. The application of anodal iontophoresis further improved NYST flux. Conversely, NYST transungual permeation was not influenced by TW80 either in the passive diffusion or iontophoretic flux. Furthermore, the iontophoretic treatment does not appear to induce irreversible alterations to the hoof bovine membranes. The present work demonstrated the efficacy of iontophoresis as a treatment for different nail pathologies with large molecules very slightly soluble in water without irreversibly affecting the nail structure. A synergistic effect between CPC and iontophoresis was observed.

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“…FSD size reduction could be considered a promising strategy in enhancing the solubility and accordingly the dissolution rate and drug bioavailability. Different formulations have been reported to enhance FSD bioavailability, through oral and non-oral routes, especially when the drug is formulated in a nanostructured systems (Monti et al., 2014 ; Tampucci et al., 2014 ). Also, drug disposition and intracellular activity on BPH cells could be improved when employing the same technique.…”

Section: Introductionmentioning

confidence: 99%

Effect of finasteride particle size reduction on its pharmacokinetic, tissue distribution and cellular permeation

Ahmed

Al‐Abd

2018

Drug Delivery

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Finasteride (FSD), a specific competitive inhibitor of the steroid type-II 5α-reductase enzyme, is used in treatment of benign prostate hyperplasia (BPH) and male pattern baldness. The drug is of limited solubility that affect its dissolution and bioavailability. The aim was to study the effect of FSD particle size reduction on the pharmacokinetic, tissue distribution and cellular permeation. An optimized drug micro- and nano-particles were developed, characterized, administered to group of rats, and systemic pharmacokinetic and tissue distribution within target and not-target organs were determined using near-infrared (NIR) spectroscopy technique. Moreover, the cellular permeation of the prepared formulations through normal prostate epithelial cells was assessed and compared to pure FSD. The developed micro- and nano-particles were of 930 and 645 nm, respectively. Plasma maximum drug levels (Cmax) and overall exposure (AUC) of both formulations were not significantly higher than unformulated drug. However, micronized FSD achieved significant higher concentration within the target tissue (prostate) within the current study compared to pure drug and nano-sized formulation as well. Yet, this is explained by the higher sequestration ability of spleen tissue to the nano-sized formula compared to micro-sized FSD. At the cellular level, permeation of nano-sized FSD through prostate epithelial cells was superior to the unformulated FSD as well as the micro-sized drug formulation. FSD particle size reduction significantly influences its cellular permeation and to a lesser extend affect its systemic pharmacokinetics and tissue distribution after oral administration.

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Topical Formulations Containing Finasteride. Part I: In Vitro Permeation/Penetration Study and In Vivo Pharmacokinetics in Hairless Rat

Cited by 26 publications

References 47 publications

Topical Formulations Containing Finasteride. Part II: Determination of Finasteride Penetration into Hair Follicles using the Differential Stripping Technique

Topical Formulations Containing Finasteride. Part II: Determination of Finasteride Penetration into Hair Follicles using the Differential Stripping Technique

Influence of a Combination of Chemical Enhancers and Iontophoresis on In Vitro Transungual Permeation of Nystatin

Effect of finasteride particle size reduction on its pharmacokinetic, tissue distribution and cellular permeation

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