Effect of β-sitosterol concentration and high pressure homogenization on the chlorhexidine release from vesicular gels

Farkas, Edit; Schubert, Rolf; Zelkó, Romána

doi:10.1016/j.ijpharm.2005.09.018

Cited by 7 publications

(5 citation statements)

References 20 publications

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“…Moreover, a large amount of cholesterol may cause crystallization of the carbohydrate chains, the phenomenon which has destabilization effect on liposomal formulation . In comparison, the crystals formation was not observed in liposomes with β‐sitosterol, which, as being more lipid soluble and less planar than cholesterol, could act more effectively in rearranging of the acid chains of phospholipids bilayer …”

Section: Resultssupporting

confidence: 91%

“…Despite of these beneficial properties, phytosterols have received far less attention in comparison to cholesterol. There are studies showing that phytosterols influence some membrane properties, such as permeability, thermal behavior, structural characteristics, and stability . However, the currently available literature data are scarce in systematic investigation how phytosterols (such as β‐sitosterol) affect liposomal membranes of different structure and composition, especially in comparison to cholesterol.…”

Section: Introductionmentioning

confidence: 99%

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Comparative Effects of Cholesterol and β‐Sitosterol on the Liposome Membrane Characteristics

Jovanović

Balanč

Ota

et al. 2018

Euro J Lipid Sci & Tech

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The influence of different phospholipid types (pure phospholipids 1‐palmitoyl‐2‐oleoyl‐sn‐glycero‐3‐phosphocholine, POPC, 1,2‐dipalmitoyl‐sn‐glycero‐3‐phosphocholine, DPPC, and one commercial phospholipid mixture, Lipoid H100), sterol types (cholesterol vs. β‐sitosterol), and various sterol concentrations (5–50 mol%) on liposomal membrane fluidity, thermotropic properties, liposome size, zeta potential, and lipid oxidation kinetics using fluorescent lipid probe BODIPY 581/591 C11 (4,4‐difluoro‐5‐[4‐phenyl‐1,3‐butadienyl]‐4‐bora‐3a,4a‐diaza‐s‐indacene‐3‐undecanoic acid) are investigated. DPPC bilayer is more rigid than POPC and phospholipids mixture membranes. Pure DPPC gives the smallest liposomes, while liposomes of Lipoid H100 have the largest diameter. Both sterols reduce membrane fluidity of all liposomes, increase absolute zeta potential, cause significant changes in particle size, and decrease phase transition temperature (Tm) and enthalpy of DPPC. POPC/β‐sitosterol liposomes exhibit the most significant lipid oxidation of the lipophilic probe. Along with beneficial effects of phytosterols on human health, better membrane fluidity, more favorable and stabilizing interactions with phospholipids, smaller vesicle size, and enhanced physical stability in comparison to cholesterol are some of the encouraging results for the use of β‐sitosterol in liposome formulations for potential application in foods, pharmaceutics, and cosmetics. Practical Applications: Adjusting the composition of liposomal membrane (lipid type, sterol type, and concentration) can be used as a tool to control membrane fluidity, permeability, and thermotropic properties, and thus predict release properties, physical, thermal, and oxidative stability. A commercial phospholipid mixture of different natural phospholipids with impurities creates less uniform liposomal membrane that is characterized by higher fluidity in comparison to DPPC. The type of phospholipid has huge influence on MLVs size. β‐sitosterol, which is a phytosterol with beneficial effects on human health can be used as a replacement for cholesterol in liposomal formulations, but with the following in mind: β‐sitosterol reduces fluidity of the phospholipid bilayer to a lesser extent than cholesterol, β‐sitosterol gives smaller MLVs than cholesterol, DPPC/β‐sitosterol SUVs are bigger than 100 nm in diameter (relevant for intravenous administration), MLVs with ≥30 mol% of β‐sitosterol can be considered as physically stable (unlike those with cholesterol), irrespective to the phospholipid type. The influence of different phospholipid types, sterol types, and various sterol concentrations on liposomal membrane fluidity, thermo tropic properties, liposomesize, zeta potential, and lipid oxidation kinetics are investigated.

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Section: Resultssupporting

confidence: 91%

Section: Introductionmentioning

confidence: 99%

Comparative Effects of Cholesterol and β‐Sitosterol on the Liposome Membrane Characteristics

Jovanović

Balanč

Ota

et al. 2018

Euro J Lipid Sci & Tech

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“…As my knowledge, few of the studies have been carried out on the β-sitosterol to improve the therapeutic efficacy. Most of the investigations conducted with β-sitosterol have focused on using it and its derivatives as an excipients to regulate drug release or promote drug absorption (Farkas et al., 2006 ; Lacatusu et al., 2012 ). In previous study, cyclodextrins has been used to increase the aqueous bioavailability and solubility of β-sitosterol.…”

Section: Introductionmentioning

confidence: 99%

β-Sitosterol-loaded solid lipid nanoparticles ameliorate complete Freund’s adjuvant-induced arthritis in rats: involvement of NF-кB and HO-1/Nrf-2 pathway

Zhang

Zhi-yu²,

et al. 2020

Drug Delivery

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Rheumatoid arthritis (RA), autoimmune disease that is categorized via chronic inflammation manifestation, obesity, cardiovascular risk and even enhanced the mortality and affect the 0.3 and 1% of population worldwide. The current experimental study was scrutinize the anti-arthritic effect of b-sitosterol loaded solid lipid nanoparticles (SLN) against complete Fruend adjuvant (CFA)-induced arthritis via dual pathway. Double emulsion solvent displacement method was used for the preparation of b-sitosterol solid lipid nanoparticles (SLN). CFA was used to induce arthritis and rats were divided into different groups for 28 days. Biochemical, anti-inflammatory, pro-inflammatory cytokines and inflammatory mediator were estimated, respectively. Receptor activator of nuclear factor kappa-B ligand (RANKL), signal transducer and activator of transcription-3 (STAT3) nuclear factor erythroid 2-related factor 2 (Nrf 2), Heme Oxygenase-1(HO-1) and Nuclear factor-jB (NF-jB) expression were estimated. b-sitosterol-SLN significantly (p < .001) reduced the paw edema, arthritic index and increased the body weight. b-sitosterol-SLN increased the redox status of synovium freduce the malonaldehyde (MDA) and increase superoxide dismutase (SOD), glutathione (GSH) and catalase (CAT)g level and reduced the cytokines such as tumor necrosis factor-a (TNF-a), interleukin-1b (IL-1b), interleukin-2, interleukin-6, interleukin-16, interleukin-17 and increased level of interleukin-10, Transforming growth factor beta (TGF-b). b-sitosterol-SLN significantly (p < .001) reduced the level of cyclooxygenase-2 (COX-2), prostaglandin E 2 (PGE 2), vascular Endothelial Growth Factor (VEGF) and NF-jB. b-sitosterol-SLN significantly increased the expression of HO-1,Nrf 2 and decreased the expression of NF-jB, RANKL, STAT3. In conclusion, b-sitosterol SLN showed the antiarthritic effect via suppression of NF-kB and activation of HO-1/Nrf-2 pathway.

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“…It has also been reported as a formulation additive for stable micellar formulation [201], and for novel bio-active lipid nanocarriers for stabilization and sustained release [202]. It enhances drug release from a gel preparation [203], activity in phyto-vesicle preparation [181], oral absorption efficiency [204] and the sustained release of hormone [205]. More works have been conducted with BSG for enhancing absorption of a different formulation of genes [206,207] and drugs for skin [208].…”

Section: Drug Delivery With Beta-sitosterolmentioning

confidence: 99%

Critical Analysis on Characterization, Systemic Effect, and Therapeutic Potential of Beta-Sitosterol: A Plant-Derived Orphan Phytosterol

et al. 2016

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Beta-sitosterol (BS) is a phytosterol, widely distributed throughout the plant kingdom and known to be involved in the stabilization of cell membranes. To compile the sources, physical and chemical properties, spectral and chromatographic analytical methods, synthesis, systemic effects, pharmacokinetics, therapeutic potentials, toxicity, drug delivery and finally, to suggest future research with BS, classical as well as on-line literature were studied. Classical literature includes classical books on ethnomedicine and phytochemistry, and the electronic search included Pubmed, SciFinder, Scopus, the Web of Science, Google Scholar, and others. BS could be obtained from different plants, but the total biosynthetic pathway, as well as its exact physiological and structural function in plants, have not been fully understood. Different pharmacological effects have been studied, but most of the mechanisms of action have not been studied in detail. Clinical trials with BS have shown beneficial effects in different diseases, but long-term study results are not available. These have contributed to its current status as an “orphan phytosterol”. Therefore, extensive research regarding its effect at cellular and molecular level in humans as well as addressing the claims made by commercial manufacturers such as the cholesterol lowering ability, immunological activity etc. are highly recommended.

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Effect of β-sitosterol concentration and high pressure homogenization on the chlorhexidine release from vesicular gels

Cited by 7 publications

References 20 publications

Comparative Effects of Cholesterol and β‐Sitosterol on the Liposome Membrane Characteristics

Comparative Effects of Cholesterol and β‐Sitosterol on the Liposome Membrane Characteristics

β-Sitosterol-loaded solid lipid nanoparticles ameliorate complete Freund’s adjuvant-induced arthritis in rats: involvement of NF-кB and HO-1/Nrf-2 pathway

Critical Analysis on Characterization, Systemic Effect, and Therapeutic Potential of Beta-Sitosterol: A Plant-Derived Orphan Phytosterol

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