Development of an Intranasal In Situ System for Ribavirin Delivery: In Vitro and In Vivo Evaluation.

Recently, ribavirin has demonstrated effectiveness in treating glioblastoma through intranasal administration utilizing the nose-to-brain delivery route. Enhancing ribavirin's bioavailability can be achieved by utilizing intranasal stimuli-responsive systems that create a gel on the nasal mucosa. The research examined thermosensitive, pH-sensitive, and ion-selective polymers in various combinations and concentrations, chosen in line with the current Quality by Design (QbD) approach in pharmaceutical development. Following a thorough assessment of key parameters, the optimal composition of gellan gum at 0.5%, Poloxamer 124 at 2%, and purified water with ribavirin concentration at 100 mg/mL was formulated and subjected to in vivo testing. Through experiments on male rats, the nose-to-brain penetration mechanism of the active pharmaceutical ingredient (API) was elucidated, showcasing drug accumulation in the olfactory bulbs and brain.

New Biopharmaceutical Characteristics of In Situ Systems Based on Poloxamer 407.

Thermosensitive systems based on poloxamer 407 are widely used in targeted drug delivery; however, the stability of the phase transition temperature remains insufficiently studied. This article presents the results of a study on the effect of adding polyethylene glycols (PEG) with different molecular weights and some classical gel-forming polymers on the gelation temperature of thermoreversible compositions based on poloxamer 407 in a long-term experiment. The study showed a positive effect of PEG addition with average molecular weights at concentrations of 1.5-2.0%, as well as gelling agents at a concentration below the critical gelation concentration. The proposed rheological test for studying the samples' adhesion can give an indirect forecast of the composition adhesive rate. Based on the conducted studies, three experimental binary systems based on poloxamer 407 were selected, with the addition of HPMC 0.5%, sodium alginate 0.5%, and PEG 1500 1.5%. These systems are the most promising for the further development of in situ targeted drug delivery systems.

Spray Film-Forming systems as promising topical in situ Systems: A review.

Spray film-forming systems (SFFSs) provide great potential for the treatment of various types of wounds. Such systems afford to prolong the action of active substances, to prevent cross-contamination, and to ensure accelerated wound healing. Spray films are known since the mid-20th century, and nowadays they are widely used to treat minor skin injuries, but numerous clinical cases describe their successful use in the treatment of burns, wounds, bedsores, etc. The current level of polymer development and composite synthesis has greatly expanded the possibilities of creating compositions of spray film-forming systems. Scattered information and lack of standardization of such delivery systems creates difficulties for pharmaceutical development. This review highlights most of the existing requirements and suggestions from studies to standardize the characteristics of SFFSs and classify them based on scientific sources and regulatory documentation, as well as the position of such systems in the pharmaceutical market. The search and evaluation of known characterization methods and their modifications, as well as the approval of their list (separately for development and for standardization) can potentially increase the research interest in the problem of spray film-forming systems development and contribute to the registration of new drugs and medical devices in this promising dosage form, including with its own pharmacological effect.

Development of novel darunavir amorphous solid dispersions with mesoporous carriers.

The aim of this work was to compare mesoporous carriers based on silica and magnesium aluminosilicate in the amorphous solid dispersion production. Darunavir has been selected as an active pharmaceutical ingredient that is classified as a Class 2 BCS substance and exists in two commercially available forms: crystalline ethanolate and amorphous. In the course of the study, the conditions for the preparation of amorphous samples with the selected carriers were evaluated within the framework of the most common methods for obtaining solid dispersions - hot-melt extrusion, solvent wetting, and spray drying. It was determined that the obtained dispersion properties almost completely repeat the properties of the corresponding carriers. The resulting dispersions were examined in a dissolution test and the best ones was used to formulate tablets, which were studied in an in vitro dissolution test with the original Prezista. The proposed tablet formulation showed improved dissolution compared to the original one. It was also found that silica supports have a greater positive contribution to darunavir dissolution - both ethanolate or amorphous forms.

Development of Composition and Technologies of Dental Film with Ketorolac Trometamine.

The report presents the results of the development of dental films with ketorolac trometamine based on the natural biodegradable polymers from the groups of sodium alginates and xanthan gums in combination with lightly crosslinked acrylic polymer carbopol. Physicochemical properties, such as moisture, mucoadhesion, thickness, tensile strength, disintegration in phosphate buffer were determined in obtained samples of this dosage form. A comparison of physicochemical properties of experimental samples and commercial model of dental film has allowed establishing the perspective composition of complex matrix of films with ketorolac trometamine for use in dentistry.