Lasmiditan (LAS) was formulated as a nanoemulsion based in situ gel (NEIG)with the aim of improving its oral bioavailability via application intranasally. The solubility of LAS in oils, emulsifiers, and co-emulsifiers was determined to identify nanoemulsion (NE)components. Phase diagrams were constructed to identify the area of nanoemulsification. LAS NE was formulated using the spontaneous nanoemulsification method. Four NEs (F19, F24, F31, and F34) containing 7-15 % oleic acid (OA) as an oily phase, 40-55% labrasol (LR), and transcutol (TC) as emulsifier mixture at (1:1), (2:1), (3:1), and (1:2) ratio with 30-53 % (w/w) aqueous phase, having suitable optical transparency of 95–98%, globule size of 104-140 nm and polydispersity of 0.253–0.382 were selected for ex vivo permeation study. F31 with the highest flux value (2.32 ± 0.01 mg/cm2.min) relative to the other NEs. It achieves an enhancement ratio of 3.3 as compared to LAS aqueous suspension (8% LAS) also it achieves a significantly higher value of permeability coefficient. F31 was selected for the incorporation of different percentages of pH-sensitive in situ gelling polymer (Carbopol 934) to prepare NEIGs 4,5 and 6. The gel strength, pH, gelation time, and viscosity were predicted for the prepared NEIGs. In vitro release and ex vivo, nasal permeation were determined for NEIG5, which exerts comparable release and permeation values as F31 with more residence time in order to overcome the normal nasal physiological clearance.
Clotrimazole (CLO) is an antimycotic imidazole derivative applied locally for the treatment of vaginal yeast infections. In this study, CLO was formulated as vaginal mucoadhesive hydrogel, using different types of mucoadhesive polymers to ensure prolonged contact between active ingredient and vaginal mucosa.
Physicochemical properties of the prepared formulas were evaluated as a visual inspection, pH, swelling index, spreadability, and mucoadhesive characteristics, in addition to an in-vitro drug release. The influence of type and concentration of polymers as CMC-Na (1.5, 2.5, and 3.5%w/w), carbopol 940( 0.25, 0.5, and 1 %w/w) and poloxamer 407 (15, 25, 30%w/w) on CLO release from the prepared gels were also invest
... Show MoreLiquisolid compact is the most promising technique for increasing dissolution rate and bioavailability of poorly soluble drugs.Clopidogrel bisulfate is an oral antiplatelets used for treatment and prophylaxis of cardiovacular and peripheral vascular diseases related to platelets aggreagation.Clopidogrel has low solubility at high pH media of intestine and low bioavailability of a bout 50% after oral doses.The purpose of this work was to enhance dissolution pattern of clopidogrel through its formulation into liquisolid tablets.A mathematical model was used to calculate the optimum quantities of tween 80 , carrier (Avicel PH 102) and coating material (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures.The liq
... Show MoreQuercetin, one of the flavonoids family member, can be found in many vegetables, fruits, and beverages with a noticeable nutritional pharmacological properties. This study was aimed to evaluate the ability of quercetin to inhibit lipopolysaccharide (LPS) that induced lethal toxicity in vivo, and to elucidate the importance of the quercetin as an antitumor agent in breast cancer cell line MCF-7.In vivo experiments included the effect of hesperidin and LPS on the liver and spleen of male mice. In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH), and catalase (CAT), while in the spleen, the concentration of cytokines was measured including IL-33 and TNF-α. In vitro experiments included MTT
... Show MoreObjective: The present study was aimed to develop a pH-triggered in situ gel for local release of lidocaine hydrochloride (lidocaine HCL) in the buccal cavity to improve the anesthetic effect of this amino amide drug which has very high water solubility. The formulations were introduced to the oral cavity as a spray to improve compliance and for easier administration.Methods: In this work, two grades of carbopol (934 and 940)-based in situ gel spray were designed. The formulations containing lidocaine HCl 5% were prepared by mixing different concentrations of carbopol with xanthan gum. Eight formulations were investigated and evaluated for gelation capacity, spray angle, volume of solution delivered per each actuation, rheological p
... Show MorePolymeric microsphere devices occupy a wide range in the field of controlled drug delivery. Subcutaneous injectable preparations of Poly(Lactide-co-Glycolide) (PLGA) microsphere of Daptomycine were prepared by solvent extraction/evaporation technique using different copolymers ratio and molecular weights. Four formulations were prepared (F1-F4) and characterized in term of particle size, surface morphology, bulk density and porosity in addition to the drug content. The effects of the above parameters on the in-vitro release study were evaluated. These formulas were evaluated also for their in-vivo release profile using rat (as an animal model) and
... Show MoreDuctal carcinoma in situ is the most commonly diagnosed early stage breast cancer. The efficacy of intraductally delivered poly(ethylene glycol)‐doxorubicin (PEG‐DOX) nanocarriers, composed of one or more DOX conjugated to various PEG polymers, was investigated in an orthotopic ductal carcinoma in situ‐like rat model. In vitro cytotoxicity was evaluated against 13762 Mat B III cells using MTT assay. The orthotopic model was developed by inoculating cancer cells into mammary ducts of female Fischer 344 retired breeder rats. The ductal retention and in vivo antitumour efficacy of two of the six nanocarriers (5 kDa PEG‐DOX and 40 kDa PEG‐(DOX)4) were investigated based o
This study aims to encapsulate atenolol within floating alginate-ethylcellulose beads as an oral controlled-release delivery system using aqueous colloidal polymer dispersion (ACPD) method.To optimize drug entrapment efficiency and dissolution behavior of the prepared beads, different parameters of drug: polymer ratio, polymer mixture ratio, and gelling agent concentration were involved.The prepared beads were investigated with respect to their buoyancy, encapsulation efficiency, and dissolution behavior in the media: 0.1 N HCl (pH 1.2), acetate buffer (pH 4.6) and phosphate buffer (pH 6.8). The release kinetics and mechanism of the drug from the prepared beads was investigated.All prepare
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