Background: Medicinal plants have proven their value as a source of molecules with therapeutic potential, and recent studies have shown that capsaicin has profound anticancer effects in several types of human cancers. However, its clinical use is handicapped due to its poor pharmacokinetics. This study aims to enhance capsaicin’s pharmacokinetic properties by loading the molecule into nanoliposomes model and testing its anticancer activity. Methods: Nanoliposomes were prepared using the thin-film method, and characteristics were examined followed by qualitative and quantitative analyses of encapsulation efficiency and drug loading using HPLC at different lipid/capsaicin ratios. Cell viability assay (MTT) was used to determine IC50. Results: Capsaicin-loaded nanoliposomes showed optimum characteristics of morphology, particle size, zeta potential, and stability. In vitro anticancer activity of capsaicin and capsaicin-loaded nanoliposomes were compared against MCF7, MDA-MB-231, K562, PANC1, and A375 cell lines. Capsaicin-loaded nanoliposomes showed significant improvement in anticancer activity against cancers cell lines studied (p < 0.001), with increased selectivity against cancer cells compared to capsaicin. Conclusion: The encapsulated capsaicin nanoliposomes produced an improvement in pharmacokinetics properties, enhancing the anticancer activity and selectivity compared with capsaicin. This model seems to offer a potential for developing capsaicin formulations for the prevention and treatment of cancer.
Nanotechnology is the science and technology applied in biomedical engineering, dermatology, medicine, and cosmetics for designing, production, and characterizations of particles and devices at the molecular level range from 1 to 100 nm. [1][2][3][4] As a result of internal structural rearrangement, the physical characteristics of these novel materials change such as the increase in their surface area and therefore act in a differently with the targeted biological systems. [5][6][7] This change has a pronounced and significant impact on both the formulation and the delivery system of pharmaceutical and cosmeceutical preparations. 8 Many innovative delivery systems are incorporated
Worldwide, peptic ulcer and gastritis considered to be one of the biggest health challenge, Helicobacter pylori is responsible for more than eighty percent of chronic active gastritis where continual infection remains for decennary. However, the success of commercially available drugs for the management of H. pylori has overwhelmed by antibiotic-resistant strains, especially, metronidazole and clarithromycin, therefore, an urgent need arise to search for new options for treatment with enhanced anti-H. pylori activities, while being less toxic to human cells. Naturally occurring plant products, including spices, are one of these strategies that showed activity against H.pylori. Present study aim to test the antibacterial activity of capsaicin and other pure plant-derived compounds against a standard (NCTC 11916) H. pylori strain In vitro and to test for possible synergistic effect when combined with conventional therapy. Capsaicin shows good antibacterial activity on regular antimicrobial sensitivity testing methods (Anti-MSTM) and titration checkerboard assay MIC (0.0625 mg/ml), whereas piperine MIC was (0.125 mg/ ml). While for curcumin no inhibition was found. The strain was found to be resistant to metronidazole with (MIC=250 μg/ml). When combining capsaicin with metronidazole, (FIC) Fractional inhibitory concentration values shown a synergistic effect, While the additive effect was found for capsaicin combination with piperine. Our obtained data indicate that capsaicin possesses promising anti H.pylori bioactivity and synergistic activity when combined with metronidazole but more work is necessary to examine the mechanisms by which these happened. Furthermore, it is necessary to ensure its activity against H.pylori In vivo and clinical settings.
Background Poly lactic acid and its copolymers are considered to be the preferred substrates for drug delivery devices. Poly lactic acid is a biocompatible, biodegradable and nontoxic polymer. It was approved by Food and Drug Administration and thought to be among the most attractive polymeric candidates intended for controlling drug delivery. It was utilized for the development of devices for the delivery of small molecules, proteins, genes, vaccines, anticancer drugs, and macromolecules. Objectives and methods This manuscript lists the different techniques for synthesizing poly lactic acid‐based nano and microparticles such as emulsion‐based methods, precipitation‐based methods, direct compositing methods, in situ forming micro‐particles, and microfluidic technique. Conclusions In addition, it describes the application and use of poly lactic acid in biomedical and cosmetic delivery systems.
Hyaluronic acid (HA) is an endogenous substance detected and isolated from various tissues and biological fluids. Owing to its physicochemical properties, HA contributes to many biological processes at intra-and extracellular levels, such as skin hydration, joints lubrication, and wound healing, besides its anti-inflammatory and antioxidant effects. The current review highlights the employment of exogenous HA in many aesthetic and dermatological aspects. Also, it aims to clarify the skin rejuvenating activity by compensating for the biological loss of HA with advanced age. Other positive impacts of HA on hair, nail, and overall health status were also revised. Cosmetics and cosmeceuticals that contain HA, among other active ingredients, are commercially available in different dosage forms such as gels, creams, intradermal injections, and fillers. Aesthetic enhancement is achieved via soft tissue augmentation, skin hydration level increasing, grooves refilling, and collagen and elastin biosynthesis stimulation. HA contributes to various therapeutic approaches such as gingivitis, stomatitis, ulceration, and osteoarthritis. Additionally, it has beneficial uses in dentistry due to its antioxidant and anti-inflammatory properties. The recent implication of HA following the claims that it has a rejuvenating power for the skin and many therapeutic benefits has to be thoroughly investigated and delivered by a trained expert to avoid undesirable effects.
Background: Nutrients are widely used for treating illnesses in traditional medicine. Ginger has long been used in folk medicine to treat motion sickness and other minor health disorders. Chronic non-healing wounds might elicit an inflammation response and cancerous mutation. Few clinical studies have investigated 6-gingerol’s wound-healing activity due to its poor pharmacokinetic properties. However, nanotechnology can deliver 6-gingerol while possibly enhancing these properties. Our study aimed to develop a nanophytosome system loaded with 6-gingerol molecules to investigate the delivery system’s influence on wound healing and anti-cancer activities. Methods: We adopted the thin-film hydration method to synthesize nanophytosomes. We used lipids in a ratio of 70:25:5 for DOPC(dioleoyl-sn-glycero-3-phosphocholine): cholesterol: DSPE/PEG2000, respectively. We loaded the 6-gingerol molecules in a concentration of 1.67 mg/mL and achieved size reduction via the extrusion technique. We determined cytotoxicity using lung, breast, and pancreatic cancer cell lines. We performed gene expression of inflammation markers and cytokines according to international protocols. Results: The synthesized nanophytosome particle sizes were 150.16 ± 1.65, the total charge was −13.36 ± 1.266, and the polydispersity index was 0.060 ± 0.050. Transmission electron microscopy determined the synthesized particles’ spherical shape and uniform size. The encapsulation efficiency was 34.54% ± 0.035. Our biological tests showed that 6-gingerol nanophytosomes displayed selective antiproliferative activity, considerable downregulation of inflammatory markers and cytokines, and an enhanced wound-healing process. Conclusions: Our results confirm the anti-cancer activity of PEGylated nanophytosome 6-gingerol, with superior activity exhibited in accelerating wound healing.
Cosmetics, cosmeceuticals, and variable healthcare products used parabens, among other excipients, for their preservative and antimicrobial activities. Paraben derivatives exhibit distinguished physiochemical properties that enable them to be compatible with the formulation of cosmetic agents in different dosage forms. In addition to their potency and efficacy, parabens are economically efficient as they have low‐manufacturing costs. Despite the desirable characteristics, the safety of parabens use is controversial after detecting these chemicals in various biological tissues after repetitive and long‐term use of formulations containing them. The use of parabens drew public health attention after scientific reports linked skin exposure to parabens with health issues, in particular, breast cancer. In response, worldwide authorities set regulations for the allowance concentrations of paraben to be used in variable cosmetic products.
Capsaicin (CAP) is an active component in Capsicum annuum L. known to have anti inflammatory and anticancer activity. CAP is highly lipophilic and suffers low bioavailability. Therefore, developing delivery systems that enhance solubility and bioavailability can provide more promising therapeutic applications for CAP. In the current work, CAP was complexed with β-cyclodextrin (βCD) to form capsaicin-in-β-cyclodextrin (CAP-in-βCD) inclusion complexes. Then, the CAP-in-βCD inclusion complexes were characterized and loaded into PEGylated liposomes using the thin-film hydration extrusion method. The size, charge, and polydispersity index (PDI) of the PEGylated liposomes were characterized. The levels of IL-8 production were quantified after treatment using array beads. The results of this work showed that the successful formation of inclusion complexes at 1:5 M ratio of CAP to βCD respectively. PEGylated liposomes loaded with βCD/CAP inclusion complexes (CAP-in-βCD-in-liposomes) have a hydrodynamic diameter of (181 ± 36) nm, zeta potential of (−2.63 ± 4.00) mV, encapsulation efficiency (EE) of (38.65 ± 3.70)%, drug loading (DL) of (1.65 ± 0.16)%, and a stable release profile. Both free CAP and liposomal CAP showed a significant reduction in the IL-8 production by the MDA-MB-231 and A549 cancer cell lines after treatment. In conclusion, a liposomal-based drug delivery system for CAP was achieved.
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