Explore the vast range of titles available.

Background Incidence of pulmonary aspergillosis is rising worldwide, owing to an increased population of immunocompromised patients. Notable potential of the pulmonary route has been witnessed in antifungal delivery due to distinct advantages of direct lung targeting and first-pass evasion. The current research reports biomimetic surface-active lipid-polymer hybrid (LPH) nanoparticles (NPs) of voriconazole, employing lung-specific lipid, i.e. , dipalmitoylphosphatidylcholine and natural biodegradable polymer, i.e., chitosan, to augment its pulmonary deposition and retention, following nebulization. Results The developed nanosystem exhibited a particle size in the range of 228–255 nm and drug entrapment of 45–54.8%. Nebulized microdroplet characterization of NPs dispersion revealed a mean diameter of  ≤ 5 μm, corroborating its deep lung deposition potential as determined by next-generation impactor studies. Biophysical interaction of LPH NPs with lipid-monolayers indicated their surface-active potential and ease of intercalation into the pulmonary surfactant membrane at the air-lung interface. Cellular viability and uptake studies demonstrated their cytocompatibility and time-and concentration-dependent uptake in lung-epithelial A549 and Calu-3 cells with clathrin-mediated internalization. Transepithelial electrical resistance experiments established their ability to penetrate tight airway Calu-3 monolayers. Antifungal studies on laboratory strains and clinical isolates depicted their superior efficacy against Aspergillus species. Pharmacokinetic studies revealed nearly 5-, 4- and threefolds enhancement in lung AUC, T max , and MRT values, construing significant drug access and retention in lungs. Conclusions Nebulized LPH NPs were observed as a promising solution to provide effective and safe therapy for the management of pulmonary aspergillosis infection with improved patient compliance and avoidance of systemic side-effects.

Background and objectives: The emergence of multi-drug resistant (MDR) strains of Plasmodium falciparum highlights the need to develop novel antimalarial drugs. Present study explores the in vivo antiplasmodial activity of ethanol leaf extract of Thalictrum foliolosum (ELETF) against lethal murine malaria. Methods: The acute toxicity of the extract was assessed by Limit test of Lorke. The suppressive activity of the extract was evaluated by Peter's 4 day test. In vivo preventive and curative activity of ELETF was assessed by Peter's method and Ryley and Peter's method respectively. Biochemical assays were carried out using standard methods. Results: ELETF (1000 mg/kg) exhibited considerable in vivo schizontocidal activity with 67.11% chemosuppression on Day 5. The ED50 of the extract was 579.56 mg/kg. ELETF also showed significant repository activity with 87.70% chemosuppression at 750 mg/kg, which was greater than pyrimethamine (78.78%). ELETF exhibited dose dependent chemosuppression in the curative test with maximum 70.06% chemosuppression (750 mg/kg). Maximum Mean Survival Time (MST) was 19.2±4.60 and 22.66±4.41 days respectively in the suppressive and curative test, which was extremely statistically significant (p<0.0005) in comparison to untreated control which died by Day 9 post inoculation. Biochemical analysis revealed the safety of ELETF to the hepatic and renal functions of the rodent host. Interpretation & conclusion: The study reports the antiplasmodial potential of Thalictrum foliolosum (ELETF) against Plasmodium berghei infection. The extract can be developed as a phytomedicine against malaria. Alternatively, the active components can be isolated as new lead compounds against the disease.