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1.
Colloids Surf B Biointerfaces ; 185: 110573, 2020 Jan 01.
Article in English | MEDLINE | ID: mdl-31675643

ABSTRACT

Benign prostatic hyperplasia (BPH) is a condition characterized by a benign enlargement of the prostate that interferes with the normal flow of urine. This disease is treated with the oral administration of combination therapy comprising α-blockers (tamsulosin) and 5α-reductase inhibitors (dutasteride). However, these compounds have low bioavailability. Thus, transdermal microemulsions aimed at promoting permeation and efficient targeted drug delivery through the skin are used. The objectives of this study were to obtain microemulsions of the combined doses of dutasteride and tamsulosin and evaluate their anti-hyperplastic activity in vivo. A phase diagram (4:1) was obtained for the choice of microemulsions. The microemulsions were characterized in terms of the droplet size, rheology, pH, conductivity, refractive index, in vitro release profile, and antihyperplastic effect in vivo. A method for the simultaneous quantification of drugs was developed using UV-vis spectroscopy. The microemulsions had an average size less than 116 nm, an acidic pH and low viscosity. The conductivity ranged from 6.18 to 185.2 µS/cm. The in vitro release profile was sustained for 6 h. Microemulsions promoted the reduction in the size of testosterone-dependent organs (prostate and seminal vesicles). Transdermal formulations for the treatment of BPH were obtained as a therapeutic alternative to conventional treatments.


Subject(s)
Dutasteride/therapeutic use , Emulsions/chemistry , Prostatic Hyperplasia/drug therapy , Tamsulosin/therapeutic use , Animals , Drug Liberation , Male , Phase Transition , Prostate/drug effects , Prostate/pathology , Rats, Wistar , Reproducibility of Results
2.
AAPS PharmSciTech ; 20(3): 122, 2019 Feb 25.
Article in English | MEDLINE | ID: mdl-30805739

ABSTRACT

Cutaneous leishmaniasis is a neglected parasitic disease. Treatment is preferably performed with pentavalent antimony associated or not with amphotericin B (AmB). This study aimed to develop an emulgel with different chemical enhancers of cutaneous release. Initially, AmB emulsions were obtained with the chemical promoters, oleic acid and geraniol and without promoter, then for the evaluation of the formulations, a preliminary stability study was carried out where the formulations were submitted to centrifugation, before and after the freeze-thaw cycle and analyzed appearance, color, pH, spreadability, viscosity, conductivity, droplet size, assay, in vitro release study, in vitro antileishmania activity in Leishmania major promastigotes, and macrophage toxicity in the MTT test. The emulsions were yellowish, with no signs of instability after the centrifugation test. The pH range corresponded to that of the skin, which is 4.6 to 5.8, before and after the freeze-thaw cycle, the formulations had good spreadability and did not present significant viscosity differences before and after the freeze-thaw cycle, presenting a non-Newtonian characteristic. AmB content was within the kinetic model of zero order release, the formulation of 3% AmB and 5% oleic acid (formulation 1) was chosen to proceed with the antileishmania activity test and showed potential activity against the in vitro parasite with significant reduction of cytotoxicity on murine macrophages, indicating that the formulation is promising for the treatment of cutaneous leishmaniasis.


Subject(s)
Amphotericin B/administration & dosage , Antiprotozoal Agents/administration & dosage , Leishmaniasis, Cutaneous/drug therapy , Amphotericin B/chemistry , Amphotericin B/therapeutic use , Animals , Antiprotozoal Agents/chemistry , Antiprotozoal Agents/therapeutic use , Drug Compounding , Drug Liberation , Drug Stability , Emulsions , Hydrogen-Ion Concentration , Mice , Viscosity
3.
Exp Parasitol ; 164: 49-55, 2016 May.
Article in English | MEDLINE | ID: mdl-26902606

ABSTRACT

The American Cutaneous Leishmaniasis (ACL) is an infectious disease that can be fatal. The first line of treatment is pentavalent antimonies. However, due to its potential to develop resistance, Amphotericin B (AmB) started to be used as an alternative medicine. Current treatments are limited, a fact that has led to a growing interesting in developing new therapies. This study aims to evaluate the therapeutic potential in vivo of an amphotericin B + oleic acid (OA) emulgel in the treatment of cutaneous leishmaniasis in an experimental model. Strains of Leishmania major MHOM/IL/80/Friendlin of Leishmania major were used. The animals were inoculated subcutaneously. After the development of leishmanial, nodular or ulcerative lesions, the animals were divided into three groups (control, Group A and Group B) and treated twice a day for twelve days. The weight of the animals was measured and the size of the lesions was observed. A histopathological analysis was performed with skin fragments of lesions and with the spleen of animals treated with different treatments (emulgel, AmB 3% emulgel and AmB 3% plus OA 5% emulgel). It was observed that when subjected to treatment with AmB 3% emulgel during the study period using both formulations, with enhancer and without enhancer, ulcerative lesions regress gradually or even complete cure. The quantification of the average number of parasites recovered from the inoculation site was made after the treatment in each group and the differences were considered significant. The treatment with AmB 3% and OA 5% emulgel had the best in vivo therapeutic response, showing good prospects for cutaneous leishmaniasis therapy as an alternative therapy.


Subject(s)
Amphotericin B/administration & dosage , Antiprotozoal Agents/administration & dosage , Leishmania major/drug effects , Leishmaniasis, Cutaneous/drug therapy , Amphotericin B/chemistry , Animals , Antiprotozoal Agents/chemistry , Disease Models, Animal , Female , Gels , Hydrogen-Ion Concentration , Leishmaniasis, Cutaneous/pathology , Male , Mice , Mice, Inbred BALB C , Oleic Acid , Spleen/drug effects , Spleen/pathology
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