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1.
Int J Nanomedicine ; 14: 195-204, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30636872

RESUMO

BACKGROUND: 3-(2-Nitrophenyl) propionic acid-paclitaxel (NPPA-PTX) is a paclitaxel (PTX) bioreductive prodrug synthesized by our lab. We hypothesize that NPPA-PTX can self-assemble to form nanoparticles (NPs). MATERIALS AND METHODS: In the present research, the theoretical partition coefficient (XlogP) and Hansen solubility parameters of NPPA-PTX were calculated. NPPA-PTX nanoparticles prepared by NPPA-PTX and DSPE-PEG (NPPA-PTX:DSPE-PEG =1:0.1, w/w) (NPPA-PTX@PEG NPs) were prepared and characterized. The cellular uptake, in vitro antitumor activity, in vivo targeting effect, tumor distribution, in vivo antitumor activity, and safety of NPPA-PTX@PEG NPs were investigated. RESULTS: Our results indicate that NPPA-PTX can self-assemble to form NPPA-PTX@PEG NPs. Both the cellular uptake and safety of NPPA-PTX@PEG NPs were higher than those of Taxol. NPPA-PTX@PEG NPs could target tumor tissues by a passive targeting effect. In tumor tissues, NPPA-PTX@PEG NPs could completely transform into active PTX. The in vivo antitumor activity of NPPA-PTX@PEG NPs was confirmed in MDA-MB-231 tumor-bearing nude mice. CONCLUSION: The bioreductive prodrug NPPA-PTX could self-assemble to form NPs. The safety and antitumor activity of NPPA-PTX@PEG were confirmed in our in vitro and in vivo experiments. The NPPA-PTX@PEG NPs developed in this study could offer a new way of preparing bioreductive prodrug, self-assembled NPs suitable for antitumor therapy.


Assuntos
Neoplasias da Mama/patologia , Proliferação de Células/efeitos dos fármacos , Nanopartículas/administração & dosagem , Paclitaxel/análogos & derivados , Fenilpropionatos/farmacologia , Pró-Fármacos/farmacologia , Animais , Apoptose/efeitos dos fármacos , Neoplasias da Mama/tratamento farmacológico , Feminino , Humanos , Técnicas In Vitro , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos ICR , Camundongos Nus , Paclitaxel/administração & dosagem , Paclitaxel/farmacologia , Fenilpropionatos/administração & dosagem , Pró-Fármacos/administração & dosagem , Células Tumorais Cultivadas , Ensaios Antitumorais Modelo de Xenoenxerto
3.
Artigo em Inglês | MEDLINE | ID: mdl-20061726

RESUMO

BACKGROUND: The B vitamins niacinamide and panthenol have been shown to reduce many signs of skin aging, including hyperpigmentation and redness. AIMS: To measure the facial skin effects in Indian women of the daily use of a lotion containing niacinamide, panthenol, and tocopherol acetate using quantitative image analysis. METHODS: Adult women 30-60 years of age with epidermal hyperpigmentation were recruited in Mumbai and randomly assigned to apply a test or control lotion to the face daily for 10 weeks. Effects on skin tone were measured using an image capturing system and associated software. Skin texture was assessed by expert graders. Barrier function was evaluated by transepithelial water loss measurements. Subjects and evaluators were blinded to the product assignment. RESULTS: Of 246 women randomized to treatment, 207 (84%) completed the study. Women who used the test lotion experienced significantly reduced appearance of hyperpigmentation, improved skin tone evenness, appearance of lightening of skin, and positive effects on skin texture. Improvements versus control were seen as early as 6 weeks. The test lotion was well tolerated. The most common adverse event was a transient, mild burning sensation. CONCLUSIONS: Daily use of a facial lotion containing niacinamide, panthenol, and tocopheryl acetate improved skin tone and texture and was well tolerated in Indian women with facial signs of aging.


Assuntos
Face , Hiperpigmentação/tratamento farmacológico , Niacinamida/administração & dosagem , Ácido Pantotênico/administração & dosagem , Pró-Fármacos/administração & dosagem , Vitamina E/administração & dosagem , Administração Cutânea , Adulto , Método Duplo-Cego , Esquema de Medicação , Face/patologia , Feminino , Humanos , Hiperpigmentação/patologia , Pessoa de Meia-Idade , Envelhecimento da Pele/efeitos dos fármacos , Envelhecimento da Pele/patologia
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