Aprepitant (APR) belongs to Class II of the Biopharmaceutical Classification System (BCS) because of its low aqueous solubility. The objective of the current work is to develop self-nanoemulsifying drug delivery systems (SNEDDS) of APR to enhance its aqueous solubility. Preformulation studies involving screening of excipients for solubility and emulsification efficiency were carried out. Pseudo ternary phase diagrams were constructed with blends of oil (Imwitor® 988), cosolvent (Transcutol® P), and various surfactants (Kolliphor® RH40, Kolliphor® ELP, Kolliphor® HS15). The prepared SNEDDS were characterized for droplet size and nanoemulsion stability after dilution. Supersaturated SNEDDS (super-SNEDDS) were prepared to increase the quantity of loaded APR into the formulations. HPMC, PVP, PVP/VA, and Soluplus® were used as polymeric precipitation inhibitors (PPI). PPIs were added to the formulations at 5% and 10% by weight. The influence of the PPIs on drug precipitation was investigated. In vitro lipolysis test was carried out to simulate digestion of formulations in the gastrointestinal tract. Optimized super-SNEDDS were formulated into free-flowing granules by adsorption on the porous carriers such as Neusilin® US2. In vitro dissolution studies of solid super-SNEDDS formulation revealed an increased dissolution rate of the drug due to enhanced solubility. Consequently, a formulation to improve the solubility and potentially bioavailability of the drug was developed.
Background and Aims: Fomes fomentarius (L.) Fr. (jar fungus) has been used extensively in the past by surgeons, barbers, dentists, and is therefore called surgeon's fungus. The hemostatic properties of F. fomentarius extracts are important in medicine. The aim of this study was to investigate the effect of the gel formulation obtained from Fomes Fomentarius on bleeding and clotting time in rat models. Methods: The gel was made for this purpose and a cross-linked polymer of acrylic acid was used as a gelling agent. Results: The outcomes of the characterization analysis indicate the development of a successful gel formulation with optimum characteristics. Data from the antimicrobial study showed a good inhibition zone, with the strongest values against Klebsiella pneumoniae, Candida krusei, C. tropicalis, C. guilliermondii. The gel administration shortened the hemostasis time after bleeding from skin incisions by 63.9% and tail incisions by 55.63% from the original time. For coagulation time, these results are determined as 71.56% from the original time. The gel administration shortened the coagulation time after bleeding from the tail incisions by 69.9 % from the original time.
Conclusion:Our preliminary study showed that the gel formulation obtained from F. fomentarius is a potent hemostatic agent in a rat-bleeding model.
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