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In situ gels have been developed as an innovative strategy to prolong corneal residence time and enhance drug absorption compared to traditional eye drops. Our study aimed to formulate an ophthalmic in situ gel with a combination of two thermosensitive poloxamers, P407 and P188, in an optimal ratio not only to increase the time of action but also to increase the solubility of selected antibiotics for the treatment of ophthalmic infections. Two BSC II class substances, Azithromycin and Ofloxacin, with different mechanisms of action, have been incorporated into the in situ gel system after determining their solubility. The antibiotics-loaded in situ gel formulation was evaluated for its clarity, pH, rheological properties, and gel characteristics of gelling time, temperature, and capacity. The formulation demonstrated satisfactory clarity, appropriate pH, effective gelation properties in simulated tear fluid, and suitable rheological characteristics. In addition, APIs release insight has been studied through a dissolution test, and the effectivity against sensitive and resistant bacterial strains has been proved through the antimicrobial study. Therefore, our in situ gel system based on thermosensitive poloxamers, with two hydrophobic antibiotics, AZM and OFX, can be considered a valuable approach for ophthalmic drug delivery with an enhancement of the antibiotics bioavailability through increasing the contact time with the ocular surface and enhancing patient compliance. [ABSTRACT FROM AUTHOR]

Psoriasis is an immune-mediated skin condition. There are many therapeutic options for its treatment; however, none of them is completely effective. Tapinarof is a promising new active substance; it was recently approved by the FDA for the treatment of psoriasis. The aim of our study was to prepare topical nanoformulations of the active substance to improve its bioavailability and therapeutic effect. The biocompatibility investigation of the formulations was carried out by MTT assay, and the size distribution of the preparations was investigated by DLS. In parallel, the rheological properties and the texture were examined, and the in vitro release of tapinarof was assessed by the Franz diffusion method. An in vitro wound healing assay was also carried out to study the drug's properties. Our results show that the preparations were safe on HaCaT cells. The particle size of the formulations was proven to be in the nanoscale range. In the in vitro release studies, nanogel II. showed greater release of the active substance. According to the wound healing assay, incorporation of the drug into nanoformulations increases the antiproliferative and antimigration activity of the drug. Overall, nanoformulations of tapinarof were successfully prepared, and our results suggest that they can be a useful addition to the current therapeutic practice of psoriasis. [ABSTRACT FROM AUTHOR]

Psoriasis is a chronic autoimmune skin condition characterized by red, circumscribed, scaly, and erythematous plaques that can cover large skin areas. While conventional treatments such as topical corticosteroids and systemic medications are commonly prescribed, the interest in natural remedies for psoriasis has grown due to concerns about potential side effects and the desire for alternative treatment options. Rosa × damascena Mill. is rich in bioactive compounds that possess anti-inflammatory, antioxidant, and antimicrobial properties; these properties make Rosa × damascena Mill. a promising candidate for the management of skin disorders such as psoriasis. In our previous studies, we successfully formulated and tested different topical preparations containing Rosa × damascena Mill. In this study, we investigated the correlation between the Psoriasis Area and Severity Index (PASI) and Dermatology Life Quality Index (DLQI) scores in psoriasis treatment using the abovementioned creams containing Rosa × damascena Mill. extract. Several tests were performed to study the correlation between the PASI and DLQI scores in psoriasis patients. Consequently, we were able to observe an improvement in terms of the area, induration, desquamation, and erythema; such an improvement implicitly produces an improvement in patients' quality of life. The PASI and DLQI scores showed significant progress between visits. These results confirm Rosa × damascena Mill. to be a promising candidate for the topical treatment of psoriatic lesions. [ABSTRACT FROM AUTHOR]

The development of oral insulin drug delivery systems is still an ongoing challenge for pharmaceutical technology researchers, as the formulation process has to overcome a number of obstacles due to the adverse characteristics of peptides. The aim of this study was to formulate different sodium-alginate microparticles as a possible method for oral insulin administration. In our previous studies, the method has been successfully optimized using a small model peptide. The incorporation of insulin into alginate carriers containing nonionic surfactants has not been described yet. In order to enhance the absorption of insulin through biological barriers, Labrasol ALF and Labrafil M 2125 CS were selected as permeation-enhancing excipients. They were applied at a concentration of 0.10% (v/v%), along with various combinations of the two, to increase oral bioavailability. Encapsulation efficiency showed sufficient drug incorporation, as it resulted in over 80% in each composition. In vitro dissolution and enzymatic stability test results proved that, as a pH-responsive polymer, alginate bead swelling and drug release occur at higher pH, thus protecting insulin against the harsh environment of the gastrointestinal tract. The remaining insulin content was 66% due to SIF degradation after 120 min. Permeability experiments revealed the impact of permeation enhancers and natural polymers on drug absorption, as they enhanced drug transport significantly through Caco-2 cells in the case of alginate microparticle formulations, as opposed to the control insulin solution. These results suggest that these formulations are able to improve the oral bioavailability of insulin. [ABSTRACT FROM AUTHOR]

BGP-15 is an active ingredient with many advantages, e.g., beneficial cardiovascular and anti-inflammatory effects. The transdermal administration of BGP-15 has great potential, which has not been investigated yet, despite the fact that it is a non-invasive and safe form of treatment. The aim of our study was to formulate transdermal patches containing BGP-15 and optimize the production with the Box–Behnken design of experiment. The most optimal formulation was further combined with penetration enhancers to improve bioavailability of the active ingredient, and the in vitro drug release and in vitro permeation of BGP-15 from the patches were investigated. FTIR spectra of BGP-15, the formulations and the components were also studied. The most optimal formulation based on the tested parameters was dried for 24 h, with 67% polyvinyl alcohol (PVA) content and low ethanol content. The selected penetration enhancer excipients were not cytotoxic on HaCaT cells. The FTIR measurements and SEM photography proved the compatibility of the active substance and the vehicle; BGP-15 was present in the polymer matrix in dissolved form. The bioavailability of BGP-15 was most significantly enhanced by the combination of Transcutol and Labrasol. The in vitro permeation study confirmed that the formulated patches successfully enabled the transdermal administration of BGP-15. [ABSTRACT FROM AUTHOR]

The rapid progress in biotechnology over the past few decades has accelerated the large-scale production of therapeutic peptides and proteins, making them available in medical practice. However, injections are the most common method of administration; these procedures might lead to inconvenience. Non-invasive medications, such as oral administration of bio-compounds, can reduce or eliminate pain and increase safety. The aim of this project was to develop and characterize novel melanin concentrating hormone (MCH) formulations for oral administration. As a drug delivery system, penetration enhancer combined alginate beads were formulated and characterized. The combination of alginate carriers with amphiphilic surfactants has not been described yet. Due to biosafety having high priority in the case of novel pharmaceutical formulations, the biocompatibility of selected auxiliary materials and their combinations was evaluated using different in vitro methods. Excipients were selected according to the performed toxicity measurements. Besides the cell viability tests, physical properties and complex bioavailability assessments were performed as well. Our results suggest that alginate beads are able to protect melanin concentrating hormones. It has been also demonstrated that penetration enhancer combined alginate beads might play a key role in bioavailability improvement. These formulations were found to be promising tools for oral peptide delivery. Applied excipients and the performed delivery systems are safe and highly tolerable; thus, they can improve patients' experience and promote adherence. [ABSTRACT FROM AUTHOR]