Background: Bilastine is a non-sedating, second-generation antihistamine used to treat urticaria and allergic conjunctivitis. Objective: to formulate and test bilastine as a mucoadhesive ophthalmic in situ gel in order to extend its presence at site for longer time and help treat conjunctivitis and allergic rhinitis. Methods: We prepared formulations using different concentrations of poloxamers (Poloxamer 407 (P407) and Poloxamer 188 (P188)) in combination with hydroxypropyl methyl cellulose (HPMC). The prepared formulas were evaluated for their physicochemical properties, sol-gel transition temperature, viscosity, mucoadhesive strength, drug release, and kinetic modeling. Results: The prepared in situ gels were clear and transparent, having a pH ranging from 7.4 to 7.5 and a gelation temperature between 29.5 and 34.7 °C. Increasing the concentrations of P-407 and HPMC increased viscosity, gel strength, and mucoadhesion force, but caused a decrease in gelation temperature and drug release. Formula (F 14) containing P 407/P 188/HPMC as 19/4/0.75% w/v, respectively, exhibited favorable characteristics, including optimal gelation temperature (33°C), drug content (93%), gel strength (40 sec), mucoadhesive force (6125 dyne/cm2), and 91.4% in vitro drug release over 5 hours. Conclusions: The bilastine mucoadhesive in situ gel formulation is presented as a promising ophthalmic formulation for the treatment of allergic conjunctivitis.
The 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 MoreThe present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTI
... Show MoreThe aim of this study is to formulate and evaluate ezetimibe nanoparticles using solvent antisolvent technology. Ezetimibe is a practically water-insoluble drug which acts as a lipid lowering drug that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe prepared as nano particles in order to improve its solubility and dissolution rate.
Thirty formulas were prepared and different stabilizing agents were used with different concentrations such as poly vinyl pyrrolidone (PVPK-30), poly vinyl alcohol (PVA), hydroxy propyl methyl cellulose E5 (HPMC), and poloxamer. The ratios of drug to stabilizers used to prepare the nanoparticles were 1: 2, 1:3 and 1:4.
The prepared nanoparticles
... Show MoreIn situ gel can be defined as a polymer solution administered as a liquid and when exposed to some physiologic condition such as thepH, ionic, temperature modulation or solvent and UV induced gelation undergo to phase transition to a semisolid gel. Ketotifenfumarate belongs to the histamine H1 receptor antagonists, and Ketotifen fumarate is used in the treatment of allergic conditions likeconjunctivitis and rhinitis. This work aims to study the natural polymer effects (xanthan gum,gellan gum) on the properties of pH-trigger in situ ocular gel, then compared the drug-releasing rate of optimized formula with the market ketotifen eye drop. Eightformulations (F1-F8) were prepared using different concentrations of xanthan gum, gellan gum with ca
... Show MoreItraconazole (ITZ) is an antifungal drug (BCSII) used for the treatment of local and systemic fungal infections. Furthermore, ITZ used as an antifungal prophylaxis for immunocompromised patients.
The objective of the study is to overcome the two problems of low and pH dependent solubility of ITZ by its preparation as floating microparticles.
Firstly, pH-dependent floating microparticles were prepared using oil in water solvent evaporation method, from which the best one (F7) selected as a best pH-dependent formula with composition of ITZ (200mg),EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) .Then, F7 was compared with the selected Relatively pH-independent ITZ floating microparticles formula wit
... Show MoreSelexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm wi
... Show MoreFast dissolving film can be defined as a dosage form, which when placed in the oral cavity. It will rapidly disintegrate and dissolves to release the medication for oral mucosal absorption or allow for the gastrointestinal absorption to be achieved when swallowed.
Flurbiprofen is non-steroidal anti-inflammatory agent with antipyretic and analgesic properties and can be used in low doses 8.75 mg as analgesic and anti inflammatory agent in sore throat infection. This study aims to formulate flurbiprofen as oral dissolving films, to improve the effective relief of pain with severe sore throats with little or no adverse effect.
Nine formulas were prepared using solvent-casting method, and t
... Show MoreIntroduction: Methadone hydrochloride (MDN) is an effective pharmacological substitution treatment for opioids dependence, adopted in different countries as methadone maintenance treatment (MMT) programmes. However, MDN can exacerbate the addiction problem if it is abused and injected intravenously, and the frequent visits to the MMT centres can reduce patient compliance. The overall aim of this study is to develop a novel extended-release capsule of MDN using the sol-gel silica (SGS) technique that has the potential to counteract medication-tampering techniques and associated health risks and reduce the frequent visits to MMT centres. Methods: For MDN recrystallisation, a closed container method (CCM) and hot-stage method (HSM) were conduc
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