Exploring Elastic Lipid Nanovesicles for Enhanced Skin Permeation of Whole Plant Extract: A Comprehensive Investigation

Journal of Biomedical Materials Research Part B Applied Biomaterials, Год журнала: 2025, Номер 113(1)

Опубликована: Янв. 1, 2025

A new method is developed using elastic lipid nanovesicles (ELNs) loaded with ethanolic extract of Lantana camara (LC) to enhance skin permeation plant actives. The ELNs contained cholesterol, 1, 2-distearoyl-sn-glycero-3-phosphocholine, span 80, and tween 80. Firstly, 15 formulations were produced examine critical factors likely affecting formulation characteristics. In addition, surface characteristics, vesicle size, polydispersity index, zeta potential, degree deformability, % entrapment efficiency (% EE) ELN examined. As a significant parameter, was measured (using Start-M; it highly resembles human skin). influence hydrophilic-lipophilic balance (HLB), ratio vital through Start-M. particular, the LC decreased at more extensive size ranges, 400, 350-450 nm. contrast, increased significantly smaller such as 200 100 More than 75% permeated within 8 h when surfactant (span 80:tween 80; 25%:75%). Permeation studies conducted based on HLB values revealed that 78% in 12.2, an increase HLB. Cell viability assay SK-MEL-37 cells (skin cancer) reduced by ~80% 24 h, further validating formulation. Future research could investigate long-term safety therapeutic potential these clinical settings their effectiveness delivering other plant-based extracts for transdermal applications via ELNs.

Язык: Английский

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Biomolecular dynamics in the 21st century

Biochimica et Biophysica Acta (BBA) - General Subjects, Год журнала: 2023, Номер 1868(2), С. 130534 - 130534

Опубликована: Дек. 6, 2023

The relevance of motions in biological macromolecules has been clear since the early structural analyses proteins by X-ray crystallography. Computer simulations have applied to provide a deeper understanding dynamics 1976, and are now standard tool many labs working on structure function biomolecules. In this mini-review we highlight some areas current interest active development for simulations, particular all-atom molecular simulations.

Язык: Английский

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Effects of Lipid Headgroups on the Mechanical Properties and In Vitro Cellular Internalization of Liposomes

Langmuir, Год журнала: 2025, Номер unknown

Опубликована: Янв. 20, 2025

We performed all-atom and coarse-grained simulations of lipid bilayer mixtures the unsaturated DOPC, with saturated lipids having same 18-carbon acyl tails different headgroups, to understand their mechanical properties. The secondary were DSPG, DSPA, DSPS, DSPC, DSPE. DOPC:DSPG system 65:35 molar ratio was softest, area compressibility modulus KA ∼ 22% smaller than pure DOPC value. Raising mole % leads increases in KA, yet at any given composition trend is DSPG < DSPA DSPS DSPC Lipid-lipid interactions are weaker stronger DSPE systems. head phosphate groups interact strongly salt ions. Adding more ordered relative No evidence phase separation or inhomogeneities observed our simulations. synthesized three liposomal formulations, L-DOPC (pure DOPC) L-DOPC/DSPG L-DOPC/DSPA, both 15 mol lipid. L-DOPC/DSPA had approximately 3- 2-times higher vitro internalization by normal epithelial (EpH4-Ev) metastatic breast cancer (4T1) cells, compared L-DOPC. uptake EpH4-Ev cells almost 2-fold L-DOPC, but liposomes similar uptakes cells. As have values, we presumed that properties, possibly combination negative surface charges differences effective liposome diameters diffusivities, contributed these observations.

Язык: Английский

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Bile Salts Trigger Deformability in Liposomal Vesicles through Edge-Activating Action

Molecular Pharmaceutics, Год журнала: 2025, Номер unknown

Опубликована: Май 22, 2025

This study investigates how bile-salt-based edge activators (EAs) (sodium cholate, NaC; sodium deoxycholate, NaDC; and taurocholate, NaTC) can influence the mechanical properties deformability of liposomal vesicles. We have elucidated their effect on liposomes composed l-α-phosphatidylcholine (SPC). Liposomes were formulated using thin-film hydration characterized scattering, spectroscopic, atomic force microscopic (AFM) techniques. Our data show that bile salts alter hydrodynamic diameter (Dh), morphology, characteristics Their Young's modulus vesicles followed order NaDC ≥ NaC > NaTC. Breakthrough events noticed in at specific depth levels during force-deformation force-indentation experiments. Based lack hysteresis approach-retract curve, we inferred attained elasticity lower concentrations NaDC. Hydrophobic interactions between phospholipids verified from Fourier-transformed infrared spectrophotometer (FTIR) Increase salt concentration was accompanied by a red shift acyl chain (asymmetric stretching CH2 symmetric CH3) phosphate groups. suggests enhanced hydrogen bonding salts. The affinity for SPC molecule correlated with relative hydrophobicity. conclude indeed improve ability to penetrate biological barriers.

Язык: Английский

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Enhancing the Biopharmacological Characteristics of Asperosaponin VI: Unveiling Dynamic Self-Assembly Phase Transitions in the Gastrointestinal Environment

International Journal of Nanomedicine, Год журнала: 2023, Номер Volume 18, С. 7335 - 7358

Опубликована: Дек. 1, 2023

Purpose: Asperosaponin VI (ASP VI) as an active ingredient of Dipsacus asperoides , which has a wide range biological and pharmacological activity. However, its development application are restricted due to the poor gastrointestinal permeability oral bioavailability. This investigation aims reveal influence self-assembled structure by interaction between ASP endogenous components NaTC and/or DOPC in environment on biopharmaceutical properties, novelty elucidated molecular mechanism for formation nanomicelles. Methods: change phase state fluids is characterized dynamic light scattering (DLS) transmission electron microscope (TEM). UPLC-Q-TOF-MS was used analyze composition exposure nanomicelles vivo. Molecular dynamics simulation (MDS) applied preliminarily elucidate self-assembly environment. Furthermore, theS8 promoting absorption were investigated through vivo pharmacokinetic experiments, parallel artificial membrane assay (PAMPA), quadruple single-pass intestinal perfusion rats, Caco-2 cell monolayer model. Results: We demonstrated that could spontaneously form structures with sodium taurocholate (NaTC) dipalmitoyl phosphatidylcholine (DOPC) during solubilization, promoted increased vivo, thus improving biopharmacological characteristics VI. Moreover, VI-NaTC-DOPC-self-assembled nanostructures VI-NaTC-DOPC-SAN) manifested higher cellular uptake cells evidenced flow cytometry confocal microscopy, this study also revealed driven electrostatic hydrogen bonding interactions. Conclusion: provides evidence transition may play key role insoluble or low ingredients dissolution Chinese medicines. Keywords: VI, structure, environment, characteristics, bioavailability

Язык: Английский

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Quality by design (QbD) based approach for development of itraconazole loaded transferosomes for skin cancer: In vitro, ex vivo and cell line studies

Drug Development and Industrial Pharmacy, Год журнала: 2024, Номер unknown, С. 1 - 14

Опубликована: Сен. 3, 2024

Itraconazole (ITZ), a widely used systemic antifungal drug, has been ingeniously repurposed for its antitumor effects. In the present work, we have prepared and optimized ITZ-loaded transferosomes by Quality Design (QbD) approach them skin cancer.

Язык: Английский

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