Background: Dolutegravir sodium (DTG), used to treat HIV, faces challenges in delivering effective therapeutic concentrations to the brain due to the blood-brain barrier (BBB). Nanostructured lipid carriers (NLCs) combined with in situ gels present a promising strategy for enhancing brain drug delivery via the intranasal route. Objective: To compare brain pharmacokinetics of DTGs delivered via NLC-loaded in situ gel intranasal administration with the conventional intravenous (IV) drug solution. Methods: 80 Wistar rats, which were divided into three groups: two groups consisting of 39 animals each and a control group with 2 animals. Rats were administered with a dose of 1.0 mg/kg of DTGs IV, and DTGs NLC-loaded in situ gel were administered intranasally. DTGs were determined in rats’ plasma and brain tissue by high-performance liquid chromatography (HPLC). Results: Intranasal administration produced significantly higher brain drug concentrations (Cmax 35344.8ng/ml) compared to the IV solution (Cmax 4536.85ng/ml). The area under the curve (AUC) for the intranasal formulation was twice that of the IV solution, indicating enhanced bioavailability. Furthermore, the intranasal route exhibited a faster onset (lower Tmax) and prolonged retention in brain tissue. The developed nanoformulation exhibited a Drug Targeting Efficiency (DTE) of 232.5% and a Drug Targeting Potential (DTP) of 57%, suggesting improved brain targeting efficiency. Conclusions: The DTGs-loaded NLC in situ gel shows superior brain pharmacokinetics compared to IV administration, highlighting its potential as an effective strategy for enhancing brain targeting.
The corcosion behoviour of Aluminum bronze in sodium chloride solution has been studied ^tentiostatically at five temperatures in the range 293-313K.The corrosion potential shifted to more negative values with increasing temperature. The corrosion current density increased with increasing temperature. Values of Tal'el slopes and the transfer coefficients indicated hydrogen evolution reaction to occur at the cathode and mainly the dissolution at the anode.Benzotriazole (BTA) had an inhibiting effect ??? the corrosion of the Al-bronze in deaerated NaCl solution at a concentration (1*10'?- IxlO‘1) mol dm'^ over the temperature range 293-313K. Values of the protection efficiency and kinetics parameters were obtained from the corrosion current
... Show MoreThe reason for conducting this study is to prolong release of miconazole in the ocular site of action by ocular-based gels (OBGs) formulations. The formulation factors affecting on the release from OBG should be studied using various gelling agents in various concentrations to achieve the improvement in retention and residence time in response to prolonged release. In this study, the formulations were prepared using carbopol 940, pectin, sodium alginate, poloxamer 407, and poly(methacrylic acid) at 0.5%, 1%, and 1.5% w/v, respectively. Hydroxypropyl methylcellulose E5 (HPMC E5) 1% was added as thickening agent/viscosity builder. The formulation containing carbopol 940, pectin and sodium alginate at 1.5% w/v, displayed a noticable im
... Show MoreBackground: Chronic hyperglycemia is the most frequent diabetes-related metabolic disorder because of faulty insulin action or production. According to the WHO, osteoporosis is a progressive systemic skeletal disorder that decreases bone mass and micro architecture bone tissue, increasing bone fragility and fracture risk. Nervosa damage determines how much a diabetic's body is damaged. Objective: The current work aimed to examines age, BMI, HbA1c, fasting blood glucose, sclerostin, and lipid profiles (TC, TG, HDL-C, VLDL-C, and LDL-C) in Iraqi T2DM menopausal women with /without osteoporosis to detect biomarkers in such condition. Subjects and Methods: 120 subjects were included in this study. They were divided into 3 groups; Group 1 (N = 4
... Show MoreNebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formul
... Show MoreNebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formulas wit
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Sumatriptan(ST) is a selective agonist at serotonin 5-HTI receptors, as well as 5-HT1B/1D subtypes. It is effective for acute migraine attacks, but has a short half life (about 2 hours) and low oral bioavailability (15%). The purpose of this study was to develop and optimize nasal mucoadhesive in-situ gel(IG) of ST to enhance nasal residence time for migraine management. Cold method was used to prepare different formulas of ST nasal IG, using thermosensitive polymers (poloxamer 407 alone or with poloxamer 188) with a mucoadhesive polymer hyaluronic acid (HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, muc
... Show Morea porentioncsisteve has been carried out of the corrosion behavior of inconel(600) in chloride ions (Cl) over the tempreatures 293 over the temperatures 308K in both the dcacrated and the alloy
Background: An accurate adaptation of the crown to the finish line is essential to minimize cement dissolution and to preserve periodontium in fixed partial denture cases. An accurate adaptation of crown is possible only when preparation details are captured adequately in the impression and transferred to cast. For these reasons, gingival displacement is necessary to capture subgingival preparation details.The aim of the present study is to measure in vivo the horizontal displacement of the gingival sulcus obtained by using three new cordless retraction materials (Magic Foam Cord®, Racegel and Astringent Retraction Paste) in comparison to medicated retraction cord. Materials and method: Thirty-two patients requiring porcelain fused to me
... Show MoreInvasomes are newly developed types of nanovesicles. A vesicular drug delivery system is considered one of the approaches for transdermal delivery to enhance permeation and improve drug bioavailability. Ondansetron is a serotonin receptor antagonist used for treating vomiting associated with different clinical cases. The study aimed to prepare invasomal dispersions for improving permeation of ondansetron across the skin with a controlled release pattern. Twenty-seven formulas of ondansetron-loaded invasomes were prepared by a modified mechanical dispersion method. These formulas were optimized by studying the effect of variables on entrapment efficiency. Vesicle size, polydispersity, zeta potential, in-vitro release and ex-vivo perm
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