In situ composite ion-triggered gellan gum gel incorporating amino methacrylate copolymer microparticles: a therapeutic modality for buccal applicability

The aim of the current investigation is to delineate the buccal applicability of an in situ composite gel containing aceclofenac (AC) amino methacrylate copolymer microparticles (MPs), surmounting limitations of oral existing conventional therapy. AC Eudragit RL100 MPs were fabricated and statistically optimized using 2241 factorial design. Better buccal applicability and enhanced localization were achieved by combining the optimum MPs with in situ ion-activated gellan gum gel. The crosslinking and gelation of in situ gel were investigated by morphological and solid state characterizations. Suitability for buccal delivery and in vivo therapeutic efficacy in inflammation model of rats were also assessed. Results showed that the best performing formula displayed particle size (PS) of 51.00 µm and high entrapment efficiency (EE%) of 94.73%. MPs were successfully entrapped inside the gel network of the composite system. Gelation tendency, pH, shear-thinning properties and mucoadhesivity of the prepared in situ composite gel guaranteed its buccal suitability. Sustained AC release features and promising in vitro anti-arthritic response were also demonstrated. Moreover, consistent and prolonged in vivo anti-inflammatory effect was achieved, relative to standard AC. Taken together; this study proves the potential of in situ composite gel as an appropriate therapeutic proposal for AC buccal delivery

Dual buoyant/mucoadhesive macroporous polypropylene microparticles for gastric delivery of repaglinide

Preparation and characterization of dual buoyant/mucoadhesive polypropylene microparticles (MPs) loaded with repaglinide (REP) for gastric drug delivery in order to augment the weak mucoadhesion in the stomach.Porous foam powder MPs were prepared using coating polymers with variable permeability (Eudragit L100, Eudragit RSPO) alone or in combination by the soaking method. Thiolated Eudragit L100 (Eudragit L100-SH) was also synthesized and tried in an attempt to enhance the mucoadhesive properties of MPs. All formulae were characterized for their yield, flow properties, particle size, encapsulation efficiency (EE %), morphology, and drug release and its mechanistics. Possible interactions inside MPs matrix were also elucidated using FTIR study. The suitability of the selected formulae for gastroretention was evaluated by in vitro buoyancy and ex-vivo mucoadhesion studies.All REP-loaded MPs demonstrated a passable powder flow, high yield values, promising floatation and mucoadhesion. Encapsulation efficiency % values were nearly tripled upon addition of Eudragit polymers. Compared to the Eudragit free REP loaded foam powder, all formula showed more sustained release features. Eudragit L100-SH was synthesized and confirmed by FTIR. Furthermore, its incorporation, alone or in combination, exhibited a significant increase in mucoadhesion strength compared to the unmodified one.Dual buoyant/mucoadhesive MPs loaded with REP encourage planning for future in-vivo performance studies for the management of diabetes

Hyperlipidemia control using the innovative association of lupin proteins and chitosan and α-cyclodextrin dietary fibers: food supplement formulation, molecular docking study, and in vivo evaluation

A dietary supplement potentially employed for the treatment and/or prevention of hyperlipidemia was developed. The proposed product is composed of a combination of natural macromolecules as chitosan (CH), α-cyclodextrin (α-CD), and lupin proteins (LP). First, the anti-hyperlipidemic effect of the α-CD and LP binary mixture was assessed and compared to that of the extensively utilized anti-hyperlipidemic CH, using a hyperlipidemic rat model. The anti-hyperlipidemic effect of their combination was also demonstrated. Additionally, ligand–target and protein–protein docking studies were performed. The in vivo results displayed that on intergroup comparison, blending CH, α-CD, and LP promised a superior therapeutic effect over α-CD and LP mixture, CH, and the marketed atorvastatin, potentiating a considerable reduction of serum lipid profile and the calculated atherogenic risk predictor indices. Molecular docking study revealed a weak hydrophobic cholesterol–CH and cholesterol–α-CD interactions, while protein–protein docking study showed a good lipase–LP interaction, involving eight hydrogen bonds. Then, on the base of the in vivo and docking study results, a tablet formulation was produced aimed to overcome the negative technological effects of the anti-hyperlipidemic macromolecules: long disintegration time and tablets mechanical resistance. The optimized tablet formulation has a disintegration time shorter than 15 min and a weight loss from friability test lower than 1%, which are in line with the regulatory specifications for uncoated tablets. Overall, this anti-hyperlipidemic formulation is attractive for the dietary and nutraceutical market, despite further clinical studies are required to assess the efficacy, possible side effects, and product compliance

Star-shaped poly(oligoethylene glycol) copolymer-based gels: thermo-responsive behaviour and bioapplicability for risedronate intranasal delivery

The aim of this work was to obtain an intranasal delivery system with improved mechanical and mucoadhesive properties that could provide prolonged retention time for the delivery of risedronate (RS). For this, novel in situ forming gels comprising thermo-responsive star-shaped polymers, utilizing either polyethylene glycol methyl ether (PEGMA-ME 188, Mn 188) or polyethylene glycol ethyl ether (PEGMA-EE 246, Mn 246), with polyethylene glycol methyl ether (PEGMA-ME 475, Mn 475), were synthesized and characterized. RS was trapped in the selected gel-forming solutions at a concentration of 0.2% w/v. The pH, rheological properties, in vitro drug release, ex vivo permeation as well as mucoadhesion were also examined. MTT assays were conducted to verify nasal tolerability of the developed formulations. Initial in vivo studies were carried out to evaluate anti-osteoporotic activity in a glucocorticoid induced osteoporosis model in rats. The results showed successful development of thermo-sensitive formulations with favorable mechanical properties at 37 °C, which formed non-irritant, mucoadhesive porous networks, facilitating nasal RS delivery. Moreover, sustained release of RS, augmented permeability and marked anti-osteoporotic efficacy as compared to intranasal (IN) and intravenous (IV) RS solutions were realized. The combined results show that the in situ gels should have promising application as nasal drug delivery systems

Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical:improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats

Diabetes mellitus is a life-threatening metabolic disease. At the moment, there is no effective treatment available to combat it. In this study, we aimed to develop berberine-loaded bilosomes (BER-BLS) to boost the oral bioavailability and therapeutic efficacy of berberine, a natural antidiabetic medication. The BER-BLS was fabricated using a thin-film hydration strategy and optimized using a central composite design (face-centered). The average vesicle size, entrapment efficiency, and surface charge of the optimized BER-BLS preparation were 196.5 nm, 89.7%, (−) 36.4 mV, respectively. In addition, it exhibited higher stability and better-sustained release of berberine than the berberine solution (BER-SOL). BER-BLS and BER-SOL were administered to streptozocin-induced diabetic rats. The optimized BER-BLS formulation had a significant hypoglycemic impact, with a maximum blood glucose decrease of 41%, whereas BER-SOL only reduced blood glucose by 19%. Furthermore, the pharmacological effect of oral BER-BLS and BER-SOL corresponded to 99.3% and 31.7%, respectively, when compared to subcutaneous insulin (1 IU). A pharmacokinetic analysis found a 6.4-fold rise in the relative bioavailability of berberine in BER-BLS when compared to BER-SOL at a dosage of 100 mg/kg body weight. Histopathological investigation revealed that BER-BLS is suitable for oral administration. Our data demonstrate that BLS is a potential nanocarrier for berberine administration, enhancing its oral bioavailability and antidiabetic activity

Cholesterol level affects surface charge of lipid membranes in saline solution

Peer reviewe

Design and development of a reflective membrane for a novel Building Integrated Concentrating Photovoltaic (BICPV) ‘Smart Window’ system

As a new concept, Building Integrated Concentrating PV (BICPV) “smart window” system consisting of a thermotropic layer with integrated PVs is treated as an electricity-generating smart window or glazed façade. This system automatically responds to climatic conditions by varying the balance of solar energy reflected to the PV for electricity generation and transmitted through the system into the building for provision of light and heat. Its success heavily relies on the understanding of the relationship between the transmittance/reflectance properties and the composition of the thermotropic layer under different environmental temperatures. Herein, hydroxypropyl cellulose (HPC) polymer and gellan gum based hydrogel membranes with different compositions were synthesized as the reflective thermotropic layer for the smart BICPV system and their transmittance and reflectance were systematically investigated in terms of hydrogel composition and environmental temperature. Specifically, a switching temperature (Ts) of ~42 °C (6 wt. % HPC) was recorded, the measured transmittance decreases from ~ 90% to ~20%, with the temperature of the reflective layer increasing from 20°C to 60°C. No hysteresis in optical property was observed upon heating-cooling cycle of HPC membrane samples. The measured reflectivity increased with heating from ~10 % below the Ts to ~50 % above the Ts (for 6 wt. % HPC). These features indicate that the as-prepared HPC based thermotropic hydrogel layer holds great potential for application in next generation BICPV smart windows

Neuroprotective effect of ranolazine improves behavioral discrepancies in a rat model of scopolamine-induced dementia

BackgroundRanolazine (Rn), an antianginal agent, acts in the central nervous system and has been used as a potential treatment agent for pain and epileptic disorders. Alzheimer’s disease (AD) is one of the most prevalent neurodegenerative diseases and the leading factor in dementia in the elderly.AimWe examined the impact of Rn on scopolamine (Sco)-induced dementia in rats.MethodsThirty-two albino male rats were divided into four groups: control, Rn, Sco, and Rn + Sco.ResultsA significant decrease in the escape latency in the Morris water maze test after pre-treatment with Rn explained better learning and memory in rats. Additionally, Rn significantly upregulated the activities of the antioxidant enzymes in the treated group compared to the Sco group but substantially reduced acetylcholinesterase activity levels in the hippocampus. Moreover, Rn dramatically reduced interleukin-1 β (IL-1β) and IL-6 and upregulated the gene expression of brain-derived neurotrophic factor (BDNF). Furthermore, in the Sco group, the hippocampal tissue’s immunohistochemical reaction of Tau and glial factor activating protein (GFAP) was significantly increased in addition to the upregulation of the Caspase-3 gene expression, which was markedly improved by pre-treatment with Rn. The majority of pyramidal neurons had large vesicular nuclei with prominent nucleoli and appeared to be more or less normal, reflecting the all-beneficial effects of Rn when the hippocampal tissue was examined under a microscope.ConclusionOur findings indicated that Rn, through its antioxidative, anti-inflammatory, and anti-apoptotic effects, as well as the control of the expression of GFAP, BDNF, and Tau proteins, has a novel neuroprotective impact against scopolamine-induced dementia in rats

Sohair Elmowafy

Sohair Elmowafy is a nocturnal creature whose work has recently been published in The Rice Review. She holds a BA in Creative Writing, and can be found somewhere in Houston probably avoiding humans and drinking copious amounts of Coca Cola

Image processing systems for TV image tracking

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