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1.
Int J Pharm ; 663: 124564, 2024 Sep 30.
Artículo en Inglés | MEDLINE | ID: mdl-39117062

RESUMEN

PURPOSE: The present work seeks to develop, assess and refine a nanoethosomal vaginal in situ gel containing Berberine, aimed at enhancing its efficacy in treating Poly Cystic Ovary Syndrome (PCOS). This formulation aims to augment drug permeation, enable controlled release kinetics, and mitigate oral adverse effects commonly associated with Berberine administration. METHOD: Nanoethosomes formulated using diverse soya lecithin-ethanol concentrations within a 32 full-factorial-design, sought optimal formulations based on particle size and %entrapment-efficiency. Subsequent scrutiny involved PDI, Zeta potential and drug-content evaluation. TEM analysis authenticated morphology, while in vitro drug release from Nanoethosomes was examined. Pluronic F-127 concentrations (16%-21%w/v) were explored for the in situ gel, analyzing pH, gelation time and gelation temperature. The refined gel underwent evaluations for viscosity and in vitro diffusion. In vivo assessment covered pharmacokinetics, vaginal irritancy and Mifepristone-induced PCOS management, validated through histopathological and biochemical analysis, juxtaposing findings across normal, diseased, plain Berberine gel and standard metformin administered groups. RESULTS: Optimized Nanoethosomal Formulation(F3) displayed particle size of 183.5 nm, 82.58 % as %entrapment-efficiency, PDI of 0.137, -50.34 mV as zeta potential and 81.64 ± 1.57 % drug-content. TEM analysis confirmed spherical, nano-sized particles. In vitro studies exhibited 80.45 % drug release over 24 h. The formulated gel with 18 % Pluronic F-127 showed viscosity ranging from 193.01 ± 0.16cps to 1817.08 ± 1.67cps with temperature changes from 25 ± 2.0 °C to 38 ± 2.0 °C. In vitro diffusion revealed 85.99 %drug release from optimized gel. In vivo animal studies demonstrated increased plasma drug concentration, non-irritating properties in vaginal tests, and efficacy in managing Mifepristone-induced PCOS compared to other treatments. Short-term stability evaluations confirmed thermodynamic stability at room-temperature.


Asunto(s)
Berberina , Liberación de Fármacos , Síndrome del Ovario Poliquístico , Ratas Wistar , Cremas, Espumas y Geles Vaginales , Femenino , Animales , Berberina/administración & dosificación , Berberina/farmacocinética , Berberina/química , Berberina/farmacología , Síndrome del Ovario Poliquístico/tratamiento farmacológico , Cremas, Espumas y Geles Vaginales/química , Cremas, Espumas y Geles Vaginales/administración & dosificación , Vagina/efectos de los fármacos , Vagina/patología , Tamaño de la Partícula , Ratas , Administración Intravaginal , Poloxámero/química , Nanopartículas/química , Metformina/administración & dosificación , Metformina/farmacocinética , Metformina/química , Viscosidad
2.
Ther Deliv ; 14(10): 635-647, 2023 10.
Artículo en Inglés | MEDLINE | ID: mdl-38050965

RESUMEN

Aim: To develop stable non-ionic surfactant vesicles containing amisulpride (AMS) to improve brain uptake via nose to brain mechanism. Methods: Niosomes were developed using a modified ethanol injection technique, optimized using 32 factorial design and evaluated for the vesicle size (VS), percent encapsulation efficiency (EE), zeta potential (ZP) and % cumulative drug release (%CDR). Results: Optimized niosomes (Span-60: cholesterol ratio 0:1) showed 191.4 nm VS, 84.25% EE, -38.2 ZP and 81.31% CDR. In situ gel with these niosomes displayed 78% CDR. TEM analysis revealed spherical niosomes. Pharmacokinetic and brain tissue distribution studies in rats showed enhanced plasma and brain concentrations, indicating successful brain targeting. Conclusion: This strategy demonstrates improved AMS permeation via the nasal cavity, enhancing bioavailability for treating schizophrenia.


Schizophrenia is a serious mental illness causing intense symptoms like hallucinations and delusions. Medicines like amisulpride can help, but they have problems like not dissolving well. The brain's defenses also make it hard for medicines to work. People are trying to send medicine through the nose to avoid these problems. These researchers developed tiny carriers called niosomes to carry amisulpride to the brain via the nose. To further help with delivery of amisulpride to the brain, they added the niosomes to a gel that becomes solid inside the body. They found that the nisome-containing gel can keep medicine in the nose for a long time and is effective at delivering amisulpride to the brain.


Asunto(s)
Sistemas de Liberación de Medicamentos , Liposomas , Ratas , Animales , Sistemas de Liberación de Medicamentos/métodos , Portadores de Fármacos , Amisulprida , Encéfalo , Tamaño de la Partícula
3.
Curr Drug Deliv ; 20(3): 237-249, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-35400343

RESUMEN

Oral squamous cell carcinoma is a malignant disease that is causing considerable mortality worldwide. Conventional treatment approaches, like surgery, cause destructive alterations in facial appearance and oral function impairments associated with psychological and social functioning. Chemotherapy exhibits low bioaccessibility of the anticancer drugs, multiple drug resistance, higher dose necessities, which elevate toxicities to the normal cells, low therapeutic index, and non-specific targeting. Radiation therapies significantly affect the well-being of the patient and impair the quality of life. Therefore, chemotherapeutics are developed that can either actively or passively target the carcinomas, reduce the adverse side effect, and improve therapeutic efficacy. Innovations in novel drug delivery systems deliver the drugs to the desired site of action with better treatment approaches with reduced toxicities to the normal cells and improve the health and survival rate of the patient. Cancer chronotherapy enhances the treatment proficiency by administration of the drugs at the best time, considering biological timings to improve the treatment profiles. Chronotherapy provides benefits to the current anticancer therapies, with minimum adverse effects to the healthy cells. This review discusses the risk factors for oral carcinomas, targeted therapy by nanocarriers, nanotechnology approaches, the role of circadian rhythm in the management of oral cancer, and advances in controlled drug delivery.


Asunto(s)
Antineoplásicos , Carcinoma de Células Escamosas , Neoplasias de la Boca , Humanos , Cronoterapia de Medicamentos , Neoplasias de la Boca/tratamiento farmacológico , Neoplasias de la Boca/inducido químicamente , Carcinoma de Células Escamosas/tratamiento farmacológico , Calidad de Vida , Preparaciones Farmacéuticas , Sistemas de Liberación de Medicamentos , Antineoplásicos/uso terapéutico
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