BACKGROUND: It is known that a considerable number of drugs in clinical use or under development are water-insoluble drugs with poor bioavailability. The liposomal delivery system has drawn attention as one of the noteworthy approaches to increase both dissolution and absorption because of its biocompatibility and ability to encapsulate hydrophobic molecules in the lipid domain. However, several drawbacks have been reported, the most common is liposome structural instability . OBJECTIVE: To encapsulate alpha tocopherol into liposomes, to determine the new formulation stability and to study the drug-release of alpha tocopherol into the sperm cryopreservation medium. MATERIALS AND METHODS: The liposomes prepared by an ethanol injection method were characterized for size stability, alpha tocopherol release and sperm motility tests. RESULTS: The prepared unilamellar vesicles had both narrow size distribution (around 99 nm) and a good physical and chemical stability at 4°C during 12 months. The liposomes did not release the vitamin E immediately, but retained the protectant for 24 hours, probably due to the rigidity of the liposomal fence which was reinforced by adding cholesterol. Then, all vitamin E molecules were released by 48 hours. Release was potentially by Fickian diffusion probably by the creation of mini-ducts due to both agitation and fence hydration. Moreover, semen motility treated with vitamin E liposome preparations was significantly improved compared to all other treatments (including commonly used sperm conservation media). CONCLUSION : The stable vitamin E liposomes formulated in this work are a promising alternative for semen cryopreservation protection.
: Severe acute respiratory syndrome coronavirus 2 has spread rapidly since its discovery in December 2019 in the Chinese province of Hubei, reaching this day, all the continents. This scourge is, unfortunately, in lineage with various dangerous outbreaks such as Ebola, Cholera, Spanish flu, American seasonal flu. Until today, the best solution for the moment remains prevention (Social distancing, hand disinfection, use of masks, partial or total sanitary containment, etc.), there is also the emergence of drug treatment (research and development, clinical trials, use on patients). Recent reviews emphasized the role of membrane lipids in the infectivity mechanism of SARS-COV-2. Cholesterol-rich parts of cell membranes serve as docking places of host cells for the viruses. Coronavirus 2 is a member of a virus family with lipid envelope that fuses with host cell through endocytosis, internalizing its components in the cell. In vitro cell models have shown that depletion of cholesterol by cyclodextrin, and particularly methyl beta cyclodextrin disturb the host cell membrane lipid composition this way reducing the attachment of the virus to the protein receptors. This review aims to summarize the state of the art of research concerning the use of cyclodextrin or its complexes as a potential treatment against this new virus and update work already published.
Background: Camptothecin is known for a potent anticancer activity. However, its optimal activity is reduced due to its low solubility and stability in biological media. Objective: The aim of present study is to design and characterize a camptothecin (CPT) suppository formulation. Methods: Rectal suppositories of: camptothecin alone, encapsulated with cyclodextrin (CD) and in ternary system (CPT encapsulated with cyclodextrin and dispersed in polyethylene glycol (PEG) 6000) were prepared using various hydrophobic and hydrophilic polymeric bases as semi-synthetic glyceride (Suppocire® AM Pellets) and polyethylene glycols (PEGs) mixtures. Formulations were evaluated by various parameters like weight variation, drug content, hardness and liquefaction time. In vitro release study was performed in USP type I apparatus using phosphate buffer pH 7.2 as dissolution media. Results: Suppositories were within the permissible range of all physical parameters. In vitro drug released from water soluble base (PEG) was greater than that from oil soluble base with ninety percent (90%) of drug dissolution. It was also established that drug release from various formulations was by diffusion mechanism according to Higuchi’s equation. Conclusion: This new formulation offers a new approach to colorectal cancer treatment by offering an alternative and simple drug administration route.
BACKGROUND: Camptothecin (CPT) is an anticancer drug, and is not employed in the clinic because of its high hydrophobicity and low active form stability. CPT may also have potential for use in cold preservation. OBJECTIVE : To overcome these drawbacks, CPT solubility variations in the presence of cyclodextrins (CDs) and polyethylene glycol (PEG) were evaluated by Higuchi solubility experiments. MATERIALS AND METHODS: CPT was encapsulated in different cyclodextrins and polyethylene glycol using a co-evaporation method. The CPT interactions with CDs and PEG 6000 were investigated by Fourier-transformed infrared spectroscopy (FT-IR), and X-ray powder diffraction (XRPD). Then, CPT complexes were evaluated for in-vitro drug release. To evaluate the potential anticancer efficacy of the CPT complexes system, in-vitro cytotoxicity studies on human red blood cells were carried out using UV assay. The impact of the CPT complex systems on sperm motility protection during cold preservation at 4°C was studied using CASA. RESULTS: The dissolution profile of these preparations shows the improvement of the dissolution of the CPT following a fickien diffusion. The CPT solubility and stability improvement were the cause of the cytotoxicity on the red blood cells test. However, CPT alone, encapsulated, dispersed, and chemically modified protected spermatozoids during cold preservation. CONCLUSION: We confirm the interest in CPT encapsulated and dispersed in anticancer treatments. We also found that CPT encapsulated or dispersed could protect sperm against oxidative damage and improve the membrane integrity of human sperm. Consequently, CPT encapsulated our dispersed could eventually be beneficial for infertility therapy.
Nanotechnology is an emerging field in the food industry that will be important for future industrial production to address rising customer concerns and expectations for natural, nutritious, and healthful food items. People are increasingly motivated to purchase unprocessed food or even high-quality processed foods with minimum chemical additives, highlighting the need to investigate natural alternatives for commercial purposes. Natural compounds are becoming more popular among consumers since they are safer than synthetic chemical additions; however, their most functional compounds are sensitive to the adverse conditions of processing and the digestive tract, impairing their use in food matrices, and industrial-scale applications. Nowadays, nanoencapsulation of natural products can be the most suitable nanotechnology to improve stability, solubility, and bioavailability. The nanostructure can be incorporated into food during production, processing, packaging, and security. Despite the many studies on nanoencapsulation, there is still some misunderstanding about nanoencapsulation systems and preparation techniques. This review aims to categorize different nanoencapsulation techniques (chemical, physicochemical, and physicomechanical), highlight eco-friendly methods, and classify the nanoencapsulation systems as groups (polymer, lipidic and metallic). The current review summarizes recent data on the nanoencapsulation of natural compounds in the food industry that has been published since 2015 until now. Finally, this review presents the challenges and future perspectives on the nanoencapsulation of bioactive compounds in food science.
Background: Alpha-tocopherol is a potent antioxidant involved in sperm protection particularly during cryopreservation. However, its poor solubility limits the optimal protection in aqueous solutions. Objective: The aim of this study was to enhance the solubility of α-tocopherol by the use of liposomes. Methods: The experimental approach consisted to load vitamin E in liposomes prepared by ethanol injection method and the optimization carried out by an experimental design. The optimum solution was characterized by high performance liquid chromatography and scanning electron microscope. Finely, the impact on sperm motility protection was studied by the freezing technic of bovine sperm. Results: The optimum solution was obtained when using 10.9 mg/ml of phospholipids, 1.7 mg/ml of cholesterol and 2 mg/ml of vitamin E. The liposome size was 99.86 nm, providing 78.47% of loaded efficiency. The results showed also a significant positive impact on sperm motility after hours of preservation. Conclusion: In conclusion, the current results showed the interest of liposome preparation as an alternative to enhance vitamin E solubility and to protect spermatozoa during cryopreservation.
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