An esterase-activatable prodrug formulated liposome strategy: potentiating the anticancer therapeutic efficacy and drug safety

Liposomal nanomedicine represents a common and versatile carrier for the delivery of both lipophilic and hydrophilic drugs. However, the direct formulation of many chemotherapeutics into a liposomal system remains an...

Remodeling immune microenvironment in periodontitis using resveratrol liposomes as an antibiotic-free therapeutic strategy

Background Periodontitis is a complicated inflammatory disease that damages the tooth-supporting tissues, with limited pharmacotherapy available. Macrophage-targeting therapy is promising for inflammatory diseases. Resveratrol (RSV), a nonflavonoid polyphenol, is known for its anti-inflammatory and immunomodulatory effects. However, its medical application is limited by its poor stability and water-solubility, as well as its low bioavailability. Result A therapeutic resveratrol-loaded liposomal system (Lipo-RSV) was developed to treat periodontitis. The physical properties of Lipo-RSV and its ability to regulate macrophages were investigated. The results showed that Lipo-RSV had good biocompatibility and could re-educate the inflammatory macrophages from M1- to M2-like phenotype through activating p-STAT3 and downregulating p-STAT1. Besides, the Lipo-RSV could scavenge ROS and inhibit the NF-κB signal and inflammasomes, thereby reducing the pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Conclusion These results revealed that Lipo-RSV could be a potential therapeutic system for the antibiotic-free treatment for periodontal diseases. Graphical Abstract

Scolicidal and Apoptotic Activities of 5-hydroxy-1, 4-naphthoquinone as a Potent Agent against Echinococcus granulosus Protoscoleces

Cystic hydatid disease (CHD) is a zoonotic disease with different clinical stages caused by the larval stage of the cestode Echinococcus granulosus. It is important to highlight as a public health problem in various regions of the world. In the current study, the efficacy and apoptotic activity of the liposomal system containing juglone (5-hydroxy-1,4-naphthoquinone) were assessed against protoscoleces (PSCs) in vitro. To this aim, firstly, liposomal vesicles were prepared by the thin-film method. Their physico-chemical features were assessed using Zeta-Sizer and Scanning Electron Microscope (SEM). Subsequently, various concentrations (50, 100, 200, 400, and 800 μg/mL) of juglone nanoliposomes at different exposure times (15, 30, 60, and 120 min) were used against PSCs. Results showed that juglone nanoliposomes at all tested concentrations induced scolicidal effect, however, 800 μg/mL and 400 μg/mL of juglone nanoliposomes could reach 100% mortality in 60 and 120 min, respectively. Additionally, we found that caspase-3 mRNA expression was higher in PSCs treated with juglone nanoliposomes compared to control groups (p < 0.001). Therefore, juglone nanoliposomes are suggested to have a more potent apoptotic effect on PSCs. Generally, optimized doses of juglone nanoliposomes could display significant scolicidal effects. Moreover, further in vivo studies are required to evaluate the efficacy of this nanoliposome.

Green synthesis of nano-liposomes containing Bunium persicum and Trachyspermum ammi essential oils against Trichomonas vaginalis

Background: Trichomonas vaginalis, a parasitic flagellated protozoan, is one of the main non-viral sexually-transmitted diseases worldwide. Treatment options for trichomoniasis are limited to nitroimidazole compounds. However, resistance to these drugs has been reported, which requires the development of new anti-Trichomonas agents that confer suitable efficacy and less toxicity.Methods: In the present work, we assessed the effectiveness of the liposomal system containing essential oils of Bunium persicum and Trachyspermum ammi against T. vaginalis in vitro. Liposomal vesicles were prepared with phosphatidylcholine (70%) and cholesterol (30%) using the thin-film method. The essential oils of B. persicum and T. ammi were loaded into the liposomes using the inactive loading method. Liposomal vesicles were made for two plants separately. Their physicochemical features were tested using Zeta-Sizer, AFM and SEM. The anti-Trichomonas activity was determined after 12 and 24 hours of parasite cultures in TYI-S-33 medium. Results: After 12 and 24 hours of administration, the IC50 of the B. persicum essential oil nano-liposomes induced 14.41 µg/mL and 45.19 µg/mL, respectively. The IC50 of T. ammi essential oil nano-liposomes induced 8.08 µg/mL and 25.81 µg/mL, respectively. Conclusions: These data suggested that nano-liposomes of the essential oils of B. persicum and T. ammi may be a promising alternative to current treatments for Trichomonas infection.

Development and Characterization of Soy Lecithin Liposome as Potential Drug Carrier Systems for Codelivery of Letrozole and Paclitaxel

In the present work, a dual-drug-loaded soy lecithin liposomal system was developed by coencapsulation of Letrozole (LET) with Paclitaxel (PTX) to improve the efficacy in breast cancer therapy. Liposomes were synthesized by the thin film layer hydration. To sufficiently evaluate the characteristics of these liposomes, the particle size, zeta potential, morphology, drug encapsulation, in vitro drug release, and cytotoxicity were ascertained. Results showed promisingly anticancer potentials, as the following parameters indicated: nanosize diameter (around 193 nm) and negative surface charge. Data collected from the coloaded drug liposomes showed suitable encapsulation efficiency (50.56% for PTX and 31.13% for LET). Controlled and sustained releases were achieved up to 72 h for both the loaded drugs following the diffusion mechanism. In addition, the in vitro cytotoxicity study on the human breast cancer cell line (MCF-7) given the dual-drug-loaded liposome showed greater inhibition of cell growth than the single drug. Consequently, LET and PTX coloaded liposomes made from soy lecithin are expected to be an ingenious drug-delivery system for combination chemotherapy.

Green synthesis of nano-liposomes containing Bunium persicum and Trachyspermum ammi essential oils against Trichomonas vaginalis

Background: Trichomonas vaginalis, a parasitic flagellated protozoan, is one of the main non-viral sexually-transmitted diseases worldwide. Treatment options for trichomoniasis are limited to nitroimidazole compounds. However, resistance to these drugs has been reported, which requires the development of new anti-Trichomonas agents that confer suitable efficacy and less toxicity.Methods: In the present work, we assessed the effectiveness of the liposomal system containing essential oils of Bunium persicum and Trachyspermum ammi against T. vaginalis in vitro. Liposomal vesicles were prepared with phosphatidylcholine (70%) and cholesterol (30%) using the thin-film method. The essential oils of B. persicum and T. ammi were loaded into the liposomes using the inactive loading method. Liposomal vesicles were made for two plants separately. Their physicochemical features were tested using Zeta-Sizer, AFM and SEM. The anti-Trichomonas activity was determined after 12 and 24 hours of parasite cultures in TYI-S-33 medium. Results: After 12 and 24 hours of administration, the IC50 of the B. persicum essential oil nano-liposomes induced 14.41 µg/mL and 45.19 µg/mL, respectively. The IC50 of T. ammi essential oil nano-liposomes induced 8.08 µg/mL and 25.81 µg/mL, respectively. Conclusions: These data suggested that nano-liposomes of the essential oils of B. persicum and T. ammi may be a promising alternative to current treatments for Trichomonas infection.

Green synthesis of nano-liposomes containing Bunium persicum and Trachyspermum ammi essential oils against Trichomonas vaginalis

Background: Trichomonas vaginalis, a parasitic flagellated protozoan, is one of the main non-viral sexually-transmitted diseases worldwide. Treatment options for trichomoniasis are limited to nitroimidazole compounds. However, resistance to these drugs has been reported, which requires the development of new anti-Trichomonas agents that confer suitable efficacy and less toxicity.Methods: In the present work, we assessed the effectiveness of the liposomal system containing essential oils of Bunium persicum and Trachyspermum ammi against T. vaginalis in vitro. Liposomal vesicles were prepared with phosphatidylcholine (70%) and cholesterol (30%) using the thin-film method. The essential oils of B. persicum and T. ammi were loaded into the liposomes using the inactive loading method. Liposomal vesicles were made for two plants separately. Their physicochemical features were tested using Zeta-Sizer, AFM and SEM. The anti-Trichomonas activity was determined after 12 and 24 hours of parasite cultures in TYI-S-33 medium. Results: After 12 and 24 hours of administration, the IC50 of the B. persicum essential oil nano-liposomes induced 14.41 µg/mL and 45.19 µg/mL, respectively. The IC50 of T. ammi essential oil nano-liposomes induced 8.08 µg/mL and 25.81 µg/mL, respectively. Conclusions: These data suggested that nano-liposomes of the essential oils of B. persicum and T. ammi may be a promising alternative to current treatments for Trichomonas infection.