RESUMEN
Burn wounds are a complicated process with ongoing psychological and physical issues for the affected individuals. Wound healing consists of multifactorial molecular mechanisms and interactions involving; inflammation, proliferation, angiogenesis, and matrix remodeling. Amlodipine (ADB), widely used in cardiovascular disorders, demonstrated antioxidant and anti-inflammatory effects in some non-cardiovascular studies. It was reported that amlodipine is capable of promoting the healing process by regulation of collagen production, extracellular matrix, re-epithelialization and wound healing through its vasodilation and angiogenic activity. The objective of the current study is to appraise the wound healing capacity of amlodipine-loaded SLN (ADB-SLN) integrated into a hydrogel. The in-vitro characterization revealed that the optimized formulation was nanometric (190.4 ± 1.6 nm) with sufficiently high entrapment efficiency (88 % ± 1.4) and sustained ADB release (85.45 ± 4.45 % after 12 h). Furthermore, in-vivo evaluation was conducted on second-degree burns induced in male Sprague-Dawley rats. ADB-SLN gel revealed a high wound contraction rate and a significant improvement in skin regeneration and inflammatory biomarkers levels, confirming its efficiency in enhancing wound healing compared to other tested and commercial formulations. To conclude, the present findings proved that ADB-SLN integrated hydrogel offers a promising novel therapy for burn wound healing with a maximum therapeutic value.
Asunto(s)
Amlodipino , Quemaduras , Nanopartículas , Ratas Sprague-Dawley , Cicatrización de Heridas , Animales , Quemaduras/tratamiento farmacológico , Masculino , Cicatrización de Heridas/efectos de los fármacos , Amlodipino/administración & dosificación , Lípidos/química , Ratas , Hidrogeles/administración & dosificación , Hidrogeles/química , Liberación de Fármacos , Portadores de Fármacos/química , Piel/efectos de los fármacos , Piel/metabolismo , LiposomasRESUMEN
Berberine (Brb) and piperine (Pip) are salient examples of bioactive nutraceuticals possessing a promising role in controlling epilepsy. However, during the development of novel nanoformulation that augments their effects, an adequate determination of each one separately was a challenge since they have nearly the same detection wavelength and diverse solubility profiles. Consequently, a tailored high-performance liquid chromatography technique was developed for their simultaneous detection in routine analyses. The chromatographic separation was achieved using a C18 column. The linear gradient flow of acetonitrile: 0.1%v/v aqueous phosphoric acid was altered from 55:45 to 80:20 v/v over 3 min at a 1.2 mL/min flow rate until the end of the run. Brb and Pip were eluted at 1.6 and 3.4 min, respectively. The linearity of the standard curves was found to be ≥0.999, and the mean % recovery for Brb and Pip lay within the accepted limit. Moreover, the percentage coefficient of variation was <2% for intra- and inter-day precision. Consequently, the developed assay was successfully applied for the quantification of both drugs rapidly with high resolution and minimum interference from each other during the different steps conducted during the nanoformulation development.
Asunto(s)
Alcaloides , Berberina , Piperidinas , Alcamidas Poliinsaturadas , Berberina/análisis , Cromatografía Líquida de Alta Presión/métodos , Alcaloides/química , Benzodioxoles , Reproducibilidad de los ResultadosRESUMEN
PURPOSE: This work aimed to fabricate alginate based in-situ gelling matrix of vildagliptin improved by calcium and carboxy methyl cellulose (CMC) for appropriate adjustment of the onset and duration of action. This easy-to-swallow thickened liquid preparation aimed to improve compliance for dysphagic or elderly diabetic patients. METHODS: Vildagliptin dispersions containing alginate were fabricated in the presence or absence of calcium chloride to assess the effect of calcium ion, then a matrix containing 1.5% w/v of sodium alginate with calcium was further examined after the addition of CMC with different concentrations ranging from 0.1% to 0.3%. The viscosity, gelling forming property, Differential scanning calorimetry, and in-vitro drug release were assessed before monitoring the hypoglycemic effect of the selected formulation. RESULTS: In-situ gel matrixes were fabricated at gastric pH with and without calcium ions. The best formula concerning viscosity and the gel-forming property was achieved with higher CMC concentrations, which in turn decreased the rate of vildagliptin release in stimulated gastric pH. In-vivo results confirmed the extended hypoglycemic effect of the vildagliptin in-situ gelling matrix compared to the vildagliptin aqueous solution. CONCLUSION: This study represents a green polymeric-based in-situ gel as a liquid oral retarded release preparation intended for reducing dose frequency, easier administration of vildagliptin, and improving compliance in geriatric and dysphagic diabetic patients.
Asunto(s)
Diabetes Mellitus , Polímeros , Humanos , Anciano , Preparaciones de Acción Retardada/química , Vildagliptina , Calcio/química , Viscosidad , Hipoglucemiantes/uso terapéutico , Alginatos/química , Geles/químicaRESUMEN
Berberine hydrochloride is a plant alkaloid with versatile medicinal applications, yet it has suffered from multiple limitations in its usage. Nonetheless, the acknowledged role of berberine in controlling seizures has fuelled the need to develop a nanosystem capable of delivering it safely and efficiently to the brain. Consequently, zein and hyaluronic acid were chosen for this purpose, and about twenty formulations with different preliminary factors were screened. Afterward, three promising formulations were loaded with berberine and characterized to select an optimum formulation for further in vivo inspection. The B2 formula of particle size of 297.2 nm ± 1.86 and % entrapment efficiency of 83.75% ± 1.39 has succeeded in the increment of the brain uptake of berberine. Moreover, compared to free berberine suspension, the severity of pilocarpine-induced status epilepticus in rats was depleted after the subcutaneous administration of B2. The hippocampal tissue of rats receiving B2 showed signs of reduced neuro-degeneration, remarkably lower expression levels of COX-2 and TNF-α, and enhanced antioxidant activity. Finally, the relative safety of the developed system was determined after searching for any sign of intoxication or behavioral changes. In conclusion, the developed berberine loaded composite nanoparticles successfully delivered berberine across the BBB securely to ameliorate the deteriorating impact of pilocarpine-induced epilepsy.
Asunto(s)
Berberina , Epilepsia , Nanopartículas , Zeína , Ratas , Animales , Ácido Hialurónico , Pilocarpina , Encéfalo , Epilepsia/inducido químicamente , Epilepsia/tratamiento farmacológicoRESUMEN
Ocular inflammation is a natural defensive phenomenon, but, it results in discomfort in the eye; as well as makes the eye vulnerable to other diseases. The aim of this work is to investigate that Curcumin (CUR) could be an effective safer biofreindly alternative for treatment of ocular inflammation. Complete in-vitro characterization of proniosomal gel loading-CUR using different surfactants was studied. A comparative in-vivo evaluation of selected formulation to a marketed corticosteroid drops in induced-eye inflammation model in rabbits was assessed. The selected formulation (FCr 300) composed of Cremophore RH surfactant, lecithin and cholesterol (9:9:1) loading CUR (1.2% w/w). The formulation showed mean PS(212.0 ± 0.1)nm, PDI (0.3 ± 0.1) , ZP(-5.1 ± 0.2)mV and % EE (96.0 ± 0.1). TEM showed multilamellar circular shaped niosomes with smooth surface. SEM showed ruptured vesicles for the lyophilized formula. Selected proniosomal gel showed enhanced permeability 3.22-fold and 1.76-fold higher than CUR dispersion and its lyophilized form respectively. Both proniosomal gel (FCr300) and corticosteroid drops reduced the induced inflammatory signs effectively by 40% on day-one and complete recovery on day-four. This anti-inflammatory result was confirmed by histopathological analysis after treatment. Assessment of cumulative IOP as a predicted side effect verified the goal of this work. In conclusion, the use of CUR as a natural biofreindly alternative to the current chemical conventional ocular anti-inflammatory treatment protocols is comparable as an anti-inflammatory drug with much less side effects.