An ophthalmic cyclosporine (CsA) formulation based on Lipid nanocapsules (LNC) was developed for dry eye management, aiming to provide targeting to ocular tissues with long-term drug levels and maximum tolerability. CsA-LNC were of small particle size (41.9 ± 4.0 nm), narrow size distribution (PdI ≤ 0.1), and high entrapment efficiency (above 98%). Chitosan (C) was added to impart positive charge. CsA-LNC were prepared as in-situ gels using poloxamer 407 (P). Ex vivo mucoadhesive strength was evaluated using bovine cornea, while in vivo corneal biodistribution (using fluorescent DiI), efficacy in dry eye using Schirmer tear test (STT), and ocular irritation using Draize test were studied in rabbits compared to marketed ophthalmic CsA nanoemulsion (CsA-NE) and CsA in castor oil. LNC incorporation in in-situ gels resulted in an increase in mucoadhesion, and stronger fluorescence in corneal layers seen by confocal microscopy, compared to the other tested formulations. Rate of recovery (days required to restore corneal baseline hydration level) assessed over 10 days, showed that CsA-LNC formulations produced complete recovery by day 7 comparable to CsA-NE. No Ocular irritation was observed by visual and histopathological examination. Based on data generated, CsA-LNC-CP in-situ gel proved to be a promising effective nonirritant CsA ophthalmic formulation for dry eye management.

Purpose: Lipid nanocapsules (LNCs) have shown potential to increase the bioavailability and efficacy of orally administered drugs. However, their intestinal translocation to distal target sites and their implication in pharmacokinetic (PK)–pharmacodynamic (PD) relationships are yet to be elucidated. In this study, the effect of LNCs on the PD activity and pharmacokinetics of praziquantel (PZQ), the mainstay of schistosomiasis chemotherapy, was investigated. Materials and methods: The composition of LNCs was modified to increase PZQ payload and to enhance membrane permeability. PZQ–LNCs were characterized in vitro for colloidal properties, entrapment efficiency (EE%), and drug release. PD activity of the test formulations was assessed in Schistosoma mansoni-infected mice 7 days post-oral administration of a single 250 mg/kg oral dose. Pharmacokinetics of the test formulations and their stability in simulated gastrointestinal (GI) fluids were investigated to substantiate in vivo data. Results: PZQ–LNCs exhibited good pharmaceutical attributes in terms of size (46–62 nm), polydispersity index (0.01–0.08), EE% (>95%), and sustained release profiles. Results indicated significant efficacy enhancement by reduction in worm burden, amelioration of liver pathology, and extensive damage to the fluke suckers and tegument. This was partly explained by PK data determined in rats. In addition, oral targeting of the worms was supported by the stability of PZQ–LNCs in simulated GI fluids and scanning electron microscopy (SEM) visualization of nanostructures on the tegument of worms recovered from mesenteric/hepatic veins. Cytotoxicity data indicated tolerability of PZQ–LNCs. Conclusion: Data obtained provide evidence for the ability of oral LNCs to target distal postabsorption sites, leading to enhanced drug efficacy. From a practical standpoint, PZQ–LNCs could be suggested as a potential tolerable single lower dose oral nanomedicine for more effective PZQ mass chemotherapy.

There is a growing global interest in developing greener and safer pharmaceutical formulations that minimize environmental impact. In this study, we present a biotechnological nanoformulation combining prodigiosin (PG), a water-insoluble, microbially derived red pigment with multifunctional bioactivity and surfactin (SF), a lipopeptide biosurfactant known for its diverse surface-active properties. PG was produced by Serratia marcescens, spectrally characterized, and subsequently incorporated into preformed SF nanomicelles (nSF) via thermal sonication at 50 °C, yielding PG-loaded nanomicelles (nPG/SF). Physicochemical characterization of nPG/SF revealed spherical nanostructures with an average diameter of 227 ± 18.95 nm, a moderate polydispersity index (PDI) of 0.59 ± 0.17, a negative surface charge (-27.1 ± 0.97 mV), high entrapment efficiency (98%), and physical stability at 4 °C for at least 14 days. In terms of bioactivity, nanomicellization appeared to enhance the antibacterial effect of PG against Staphylococcus aureus and a clinical isolate of Pseudomonas aeruginosa, while significantly (p < 0.05) improving SF's cytotoxic activity against two breast cancer cell lines, MCF-7 and MDA-MB-231. Furthermore, using nSF as a carrier slightly increased PG’s anticancer activity, suggesting the potential for dose reduction of both PG and SF. Overall, this study provides a proof of concept for an eco-friendly, biosurfactant-based nanomicellar PG formulation with improved solubility, stability, and bioactivity, supporting its potential in pharmaceutical and biotechnological applications. Further investigations are warranted to validate and extend these findings.