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1.
Biofactors ; 50(2): 232-249, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-37702264

RESUMEN

Piceatannol is a naturally occurring hydroxylated resveratrol analogue that can be found in a variety of fruits and vegetables. It has been documented to have a wide range of beneficial effects, including anti-inflammatory, antioxidant, anti-aging, anti-allergic, antidiabetic, neuroprotective, cardioprotective, and chemopreventive properties. Piceatannol has significantly higher antioxidant activity than resveratrol. Piceatannol has been shown in preclinical studies to have the ability to inhibit or reduce the growth of cancers in various organs such as the brain, breast, lung, colon, cervical, liver, prostate, and skin. However, the bioavailability of Piceatannol is comparatively lower than resveratrol and other stilbenes. Several approaches have been reported in recent years to enhance its bioavailability and biological activity, and clinical trials are required to validate these findings. This review focuses on several aspects of natural stilbene Piceatannol, its chemistry, and its mechanism of action, and its promising therapeutic potential for the prevention and treatment of a wide variety of complex human diseases.


Asunto(s)
Enfermedades no Transmisibles , Estilbenos , Humanos , Resveratrol/uso terapéutico , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Estilbenos/farmacología , Estilbenos/uso terapéutico , Estilbenos/química
2.
Curr Drug Deliv ; 20(6): 730-751, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-35422213

RESUMEN

The vagina is an essential part of the female reproductive system and offers many potential benefits over conventional drug delivery, including a large surface area for drug absorption, relatively low enzymatic activity, avoiding first-pass effects, and ease of administration. The vaginal mucosal cavity is an effective route for administering therapeutic agents that are intended both for local and systemic administration. The present review provides a comprehensive overview of recent trends and developments in vaginal drug delivery. Marketed formulations and products under clinical study are also reviewed. Various novel vaginal delivery systems have been studied in recent years as effective tools for delivering a range of therapeutic agents to the vagina. These systems offer numerous benefits, including sustained delivery, improved bioavailability, effective permeation, and higher efficacy. The recent focus of the scientific community is on the development of safe and efficient drug delivery systems, such as nanoparticles, microparticles, vesicular systems, vaginal rings, microneedles, etc., for vaginal application. Various factors, such as the physicochemical properties of the drugs, the volume and composition of the vaginal fluid, the pH of the vaginal fluid, the thickness of the vaginal epithelium, and the influence of sexual intercourse may influence the release of drugs from the delivery system and subsequent absorption from the vaginal route. To date, only a limited number of in vivo studies on novel vaginal DDS have been reported. Additionally, drug release kinetics under varying vaginal environments is also not well understood. More research is needed to ensure the suitability, biocompatibility, and therapeutic effectiveness of novel DDS for vaginal delivery. Although numerous strategies and interventions have been developed, clinical translation of these systems remains a challenge. The toxicity of the carrier system is also an important consideration for future clinical applications.


Asunto(s)
Sistemas de Liberación de Medicamentos , Vagina , Femenino , Humanos , Embarazo , Preparaciones Farmacéuticas , Administración Intravaginal , Parto Obstétrico
3.
Drug Deliv Transl Res ; 10(5): 1171-1190, 2020 10.
Artículo en Inglés | MEDLINE | ID: mdl-32504410

RESUMEN

Over the past two decades, polymersomes have been widely investigated for the delivery of diagnostic and therapeutic agents in cancer therapy. Polymersomes are stable polymeric vesicles, which are prepared using amphiphilic block polymers of different molecular weights. The use of high molecular weight amphiphilic copolymers allows for possible manipulation of membrane characteristics, which in turn enhances the efficiency of drug delivery. Polymersomes are more stable in comparison with liposomes and show less toxicity in vivo. Furthermore, their ability to encapsulate both hydrophilic and hydrophobic drugs, significant biocompatibility, robustness, high colloidal stability, and simple methods for ligands conjugation make polymersomes a promising candidate for therapeutic drug delivery in cancer therapy. This review is focused on current development in the application of polymersomes for cancer therapy and diagnosis. Graphical abstract.


Asunto(s)
Portadores de Fármacos , Sistemas de Liberación de Medicamentos , Neoplasias , Portadores de Fármacos/uso terapéutico , Humanos , Interacciones Hidrofóbicas e Hidrofílicas , Neoplasias/diagnóstico , Neoplasias/tratamiento farmacológico , Polímeros/uso terapéutico
4.
Drug Dev Ind Pharm ; 46(3): 365-375, 2020 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-32041433

RESUMEN

Objectives: The objective of the present work to encapsulate the resveratrol (RES) inside the chitosan-based microsponges, employing the systematic optimization by 33 Box-Behnken design for the colonic targeting.Significance: Enhanced therapeutic efficacy of RES-loaded microsponges and matrix tablets, vis-a-vis pureRES for ulcerative colitis.Methods: RES-loaded microsponges were prepared employing the systematic optimization by 33 Box-Behnken design for the colonic targeting. The best-optimizedRES-loaded microsponge was compressed in the form of a tablet, employing pectin as a matrix-forming material. The encapsulation of RES inside microsponge was confirmed by XRD, DSC and FT-IR. Further, both RES-loaded microsponges and matrix tablets were evaluated for in vitro release kinetics and further evaluated for in vivo ulcerative colitis animal model.Results: Optimization experiments was obtained as the high value of r2 (particle size = 0.9999; %EE = 0.9652; %CDR = 0.9469) inferred excellent goodness of fit. SEM revealed nearly spherical and porous nature of RES-loaded microsponges. The in vitro release kinetic showed zero-order release for RES-loaded microsponges and Korsmeyer-Peppas model for matrix tablets. The pharmacodynamic studies, in ulcerative colitis rat model, indicated better therapeutic efficacy of drug-loaded microsponges and matrix tablets, vis-a-vis pure RES. Thus, the present study advocates the potential of RES based microsponges delivered by pectin based matrix tablet, in the treatment of various colonic disorders.Conclusion: The present study proved that RES-loaded microsponges and matrix tablets based on chitosan and pectin can be the ideal delivery system for colonic delivery of RES.


Asunto(s)
Antioxidantes/administración & dosificación , Colitis Ulcerosa/tratamiento farmacológico , Sistemas de Liberación de Medicamentos , Resveratrol/administración & dosificación , Ácido Acético , Animales , Antioxidantes/farmacología , Química Farmacéutica , Quitosano/química , Colitis Ulcerosa/fisiopatología , Colon/metabolismo , Colon/fisiopatología , Modelos Animales de Enfermedad , Liberación de Fármacos , Tamaño de la Partícula , Pectinas/química , Ratas , Ratas Wistar , Resveratrol/farmacología , Comprimidos
5.
Ther Deliv ; 11(2): 97-112, 2020 02.
Artículo en Inglés | MEDLINE | ID: mdl-31914859

RESUMEN

Transport of drugs through the blood-brain barrier to the brain and the toxic effects of drugs on the healthy cells can limit the effectiveness of chemotherapeutic agents. In recent years, magnetic nanoparticles (MNPs) have received much attention as targeted therapeutic and diagnostic systems due to their simplicity, ease of preparation and ability to tailor their properties such as their composition, size, surface morphology, etc. for biomedical applications. MNPs are utilized in drug delivery, radio therapeutics, hyperthermia treatment, gene therapy, biotherapeutics and diagnostic imaging. The present review will address the challenges in brain tumor targeting and discuss the application and recent developments in brain tumor targeting using MNPs.


Asunto(s)
Neoplasias Encefálicas , Nanopartículas de Magnetita , Nanopartículas , Barrera Hematoencefálica , Encéfalo/diagnóstico por imagen , Neoplasias Encefálicas/tratamiento farmacológico , Sistemas de Liberación de Medicamentos , Humanos
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