scholarly journals Are lipid nanoparticles really superior? A holistic proof of concept study

2021 ◽  
Author(s):  
Sabrina Wiemann ◽  
Cornelia M. Keck
Keyword(s):  
Chemical Stability ◽  
Chemical Properties ◽  
Lipid Nanoparticles ◽  
Proof Of Concept ◽  
Beneficial Effects ◽  
Dermal Penetration ◽  
Physico Chemical ◽  
Nanoparticle Formulation ◽  
Dermal Drug Delivery ◽  
Dermal Application

AbstractLipid nanoparticles are a successful carrier system for dermal drug delivery. They possess various beneficial properties, i.e., increased chemical stability for chemically labile compounds, increased dermal penetration of active compounds, or skin carrying properties after dermal application due to the formation of a so-called “invisible patch.” Despite manifold studies showing these properties individually, a study that investigates if one lipid nanoparticle formulation can really combine all the above-mentioned benefits at once is not yet available. In the present study, lipid nanoparticles (NLC) were produced and characterized regarding their physico-chemical properties. The chemical stability of the incorporated active ingredient (AI) was determined, as well as the dermal penetration efficacy of the AI, and the skin carrying properties of the NLC after dermal penetration. The properties of the NLC were compared to classical formulations, i.e., AI dissolved in pure oil, an o/w cream base and a nanoemulsion. All formulations contained similar lipids and emulsifiers, which allowed for a direct comparison of the different properties. NLC were shown to provide most efficient chemical stabilization and most efficient dermal penetration for the AI. The formation of the invisible patch was shown for the NLC but not for the other formulations. Skin hydration and skin carrying properties were also most pronounced for the NLC. Results provide evidence that NLC can combine all beneficial effects that were previously described in one formulation. Thus, providing evidence that NLC are a holistically superior formulation principle when compared to other formulation principles. Graphical abstract

scholarly journals Hair Follicle Targeting and Dermal Drug Delivery with Curcumin Drug Nanocrystals—Essential Influence of Excipients

Nanomaterials ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 2323
Author(s):  
Olga Pelikh ◽  
Cornelia M. Keck
Keyword(s):  
Drug Delivery ◽  
Hair Follicle ◽  
Aqueous Solubility ◽  
Hair Follicles ◽  
Passive Diffusion ◽  
Dermal Penetration ◽  
Poorly Soluble ◽  
Long Acting ◽  
Dermal Drug Delivery ◽  
Dermal Application

Many active pharmaceutical ingredients (API) possess poor aqueous solubility and thus lead to poor bioavailability upon oral administration and topical application. Nanocrystals have a well-established, universal formulation approach to overcome poor solubility. Various nanocrystal-based products have entered the market for oral application. However, their use in dermal formulations is relatively novel. Previous studies confirmed that nanocrystals are a superior formulation principle to improve the dermal penetration of poorly soluble API. Other studies showed that nanocrystals can also be used to target the hair follicles where they create a drug depot, enabling long acting drug therapy with only one application. Very recent studies show that also the vehicle in which the nanocrystals are incorporated can have a tremendous influence on the pathway of the API and the nanocrystals. In order to elucidate the influence of the excipient in more detail, a systematic study was conducted to investigate the influence of excipients on the penetration efficacy of the formulated API and the pathway of nanocrystals upon dermal application. Results showed that already small quantities of excipients can strongly affect the passive dermal penetration of curcumin and the hair follicle targeting of curcumin nanocrystals. The addition of 2% ethanol promoted hair follicle targeting of nanocrystals and hampered passive diffusion into the stratum corneum of the API, whereas the addition of glycerol hampered hair follicle targeting and promoted passive diffusion. Propylene glycol was found to promote both pathways. In fact, the study proved that formulating nanocrystals to improve the bioefficacy of poorly soluble API upon dermal application is highly effective. However, this is only true, if the correct excipient is selected for the formulation of the vehicle. The study also showed that excipients can be used to allow for a targeted dermal drug delivery, which enables to control if API should be delivered via passive diffusion and/or as drug reservoir by depositing API in the hair follicles.

scholarly journals Physico-Chemical Properties of Soil Under Acacia Senegal (L) Willd Plantation in Sahel Zone of Nigeria

2020 ◽  
Author(s):  
Titus Ayodele Ampitan
Keyword(s):  
Bulk Density ◽  
Chemical Properties ◽  
Gum Arabic ◽  
Soil Bulk Density ◽  
Acacia Senegal ◽  
Beneficial Effects ◽  
Resistant Species ◽  
Physico Chemical ◽  
Chemical Properties Of Soils ◽  
Open Woodland

Abstract BackgroundAcacia senegal (L) Wild known as gum Arabic tree, is a nitrogen fixing tree and a drought resistant species with potentials to improve infertile soils is planted in Sahel zone of Jigawa State, Nigeria for the production of gum arabic. However, there is dearth of information on the soil physico-chemical properties under plantation. MethodsSoil samples were collected from four 30 x 30m plots in the plantation and another plot in open woodland (control). In each plot, three replicate soil samples were taken from 0-15cm, 15-30cm and 30-60cm soil depths analyzed for micro and macronutrients, while soil acidity was determined both in water and 0.01M CaCl2.ResultsThe general soil texture of the plantation is loamy sand but with slight textural differentiation under the open woodland. Results indicated that physico-chemical properties of soils under the plantation were significantly different at P < 0.05 compared with the control. The mean soil bulk density ranged from 1.6g/cm3 in the plantation to 1.8g/cm3 in the open woodland. The high values of soil bulk density might be ascribed to loss of organic matter as a result of soil erosion and animal grazing which are common occurrences. ConclusionFrom the result of the study soil physico-chemical properties under the plantation are high and have more beneficial effects on the trees unlike the open woodland.

scholarly journals Probiotic Yogurt Fortified with Chickpea Flour: Physico-Chemical Properties and Probiotic Survival during Storage and Simulated Gastrointestinal Transit

Foods ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 1144
Author(s):  
Manwinder Kaur Sidhu ◽  
Fengzhi Lyu ◽  
Thomas Patrick Sharkie ◽  
Said Ajlouni ◽  
Chaminda Senaka Ranadheera
Keyword(s):  
Chemical Properties ◽  
Gastrointestinal Transit ◽  
Viable Count ◽  
Therapeutic Level ◽  
Beneficial Effects ◽  
Probiotic Yogurt ◽  
Chickpea Flour ◽  
Physico Chemical ◽  
Water Holding ◽  
Positive Effect

In the present study, probiotic yogurt with Lactobacillus acidophilus LA5 and Bifidobacterium BB12 was produced via fortification with chickpea flour (0, 1, 2.5, 5% w/v). During refrigerated storage for five weeks, probiotics maintained a viable count above the minimum therapeutic level (106 CFU/g) in all yogurt types. Although there was no significant (p > 0.05) positive effect of chickpea flour on probiotic viability during storage, the addition of chickpea flour has beneficial effects on the viability of both probiotic species in the presence of gastric and intestinal juices, with 0.3% bile. This study also evaluated the physio-chemical properties of probiotic yogurt during storage. Some physicochemical properties of yogurt, such as water holding capacity and susceptibility to syneresis, were enhanced by the addition of chickpea flour. Hence, chickpea flour could be an attractive pulse ingredient in the production of probiotic yogurts for health-conscious consumers.

scholarly journals JERUSALEM ARTICHOKE (HELIANTHUS TUBEROSUS) FLOUR IMPACT ON BREAD QUALITY

2021 ◽  
Vol 28 (1) ◽  
Author(s):  
Aurica Chirsanova ◽  
◽  
Tatiana Capcanari ◽  
Ecaterina Gîncu ◽  
◽  
...  
Keyword(s):  
Wheat Flour ◽  
Chemical Properties ◽  
Jerusalem Artichoke ◽  
Essential Amino Acids ◽  
Matter Content ◽  
Dry Matter Content ◽  
Beneficial Effects ◽  
High Dry Matter ◽  
Physico Chemical ◽  
The Impact

Jerusalem artichoke tubers are known for their high content of nutrients, high acidity, pleasant taste and smell and beneficial effects on health. Thus, the capitalization of food products such as bread with Jerusalem artichoke flour, could be an opportunity to diversify the range of new products. The aim of this research was to elucidate the impact of added Jerusalem artichoke flour (in a concentration of 2.5%, 5%, 7.5% and 10%) in wheat flour bread on the sensory and physico-chemical properties of the finished product. Jerusalem artichoke flour has a high dry matter content and a high content of essential amino acids such as histidine, isoleucine, methionine, phenylalanine and valine. In the results we recommend the replacement of wheat flour with 5% Jerusalem artichoke flour, to obtain a product rich in micro and macronutrients with better organoleptic properties and a longer shelf life, which positively influences human health.

Development and Physico-Chemical Evaluations of Clove Oil Microemulsions

2020 ◽  
Vol 859 ◽  
pp. 62-67
Author(s):  
Suwannee Panomsuk ◽  
Natcha Porkar ◽  
Pornnapa Meerasen ◽  
Nuttapoj Kunrattanaporn ◽  
Malai Satiraphan
Keyword(s):  
Chemical Stability ◽  
Ternary Phase Diagram ◽  
Chemical Properties ◽  
Tween 80 ◽  
Storage Condition ◽  
Antimicrobial Activities ◽  
Syzygium Aromaticum ◽  
Clove Oil ◽  
Surfactant Mixture ◽  
Physico Chemical

Clove oil, extracted from dried floral buds of clove (Syzygium aromaticum), are used in topical products because it has antioxidant and antimicrobial activities. Microemulsions (ME) are stable emulsion which can be formulated by simple mixing of oil, water, surfactant and co-surfactant. The objectives of this research were to develop and evaluate clove oil-loaded ME for topical application by using Tween 80 as surfactant. Ethanol, isopropanol and propylene glycol (PG) were used as co-surfactants. Pseudo ternary-phase diagram showed that using ethanol and isopropanol provided larger ME area than using PG in all surfactant:co-surfactant ratio (SR; 1:0.5, 1:1 and 1:2). Up to 20% w/w of clove oil can be loaded in ME by using surfactant mixture of 60-80% w/w. The effects of various amounts of clove oil (5-20%) and surfactant mixture (60, 70, 80%) at SR of 1:1 on physico-chemical properties of ME were observed. All formulations are transparent with the pH values of 6.8-8.0. The droplets size of ME using ethanol and isopropanol as co-surfactant ranged from 10-100 nm while that using PG was higher. Conductivity values showed that all formulations were o/w ME. Zeta potential values revealed stable particles. For ethanol and isopropanol, ME containing 5-10% clove oil and 60-70% SM showed good physico-chemical stability. The amount of eugenol in clove oil analyzed by gas chromatographic (GC-FID) method was 82.27% v/v. The stability test of selected formulations (70% surfactant mixture at SR = 1:1) was evaluated from %eugenol remaining at room temperature and in refrigerator after 4-week storage. It was found that the amount of eugenol in the formulation was effected by the storage condition. Our results indicate that clove oil can be prepared in ME with physico-chemical stability by using Tween 80 and ethanol as surfactant system.

scholarly journals Phenylalanine Butyramide Is a New Cosmetic Ingredient with Soothing and Anti-Reddening Potential

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6611
Author(s):  
Ritamaria di Lorenzo ◽  
Antonietta Bernardi ◽  
Lucia Grumetto ◽  
Antonia Sacchi ◽  
Carmen Avagliano ◽  
...  
Keyword(s):  
Butyric Acid ◽  
Skin Diseases ◽  
Chemical Properties ◽  
Short Chain Fatty Acids ◽  
Vertical Diffusion ◽  
Beneficial Effects ◽  
Physico Chemical ◽  
Solid Form

Human skin is colonized by diverse commensal microbes, making up the skin microbiota (SM), contributing to skin integrity and homeostasis. Many of the beneficial effects aroused by the SM are exerted by microbial metabolites such as short-chain fatty acids (SCFAs), including butyric acid. The SCFAs can be used in cosmetic formulations against skin diseases to protect SM by preserving and/or restoring their natural balance. Unpleasant sensorial properties and unfavorable physico-chemical properties of butyrate strongly limit its cosmetic use. In contrast, some butyrate derivatives, including phenylalanine butyramide (C13H18N2O2, FBA), a solid form of butyric acid, are odorless while retaining the pharmacokinetic properties and safety profile of butyric acid. This study assessed the FBA’s permeation across the skin and its soothing and anti-reddening potential to estimate its cosmetic application. The dosage method used to estimate FBA’s levels was validated to be sure of analytical results. The FBA diffusion tests were estimated in vitro using a Franz-type vertical diffusion cell. The soothing action was evaluated in vivo by Colorimeter CL400, measuring the erythema index. The results suggest that the FBA represents an innovative way to exploit the benefits of butyric acid in the cosmetic fields since it cannot reach the bloodstream, is odorless, and has a significative soothing action (decrease the erythema index −15.7% after 30′, and −17.8% after 60′).

Decoration of specific sites on freeze-fractured membranes

1978 ◽  
Vol 36 (2) ◽  
pp. 140-141
Author(s):  
H. Gross ◽  
H. Moor
Keyword(s):  
Pure Water ◽  
Freeze Fracture ◽  
Chemical Properties ◽  
Surface Forces ◽  
Sulfate Pentahydrate ◽  
Copper Sulfate Pentahydrate ◽  
Physico Chemical ◽  
Water Of Hydration ◽  
Small Container ◽  
Binding Forces

Fracturing under ultrahigh vacuum (UHV, p ≤ 10-9 Torr) produces membrane fracture faces devoid of contamination. Such clean surfaces are a prerequisite foe studies of interactions between condensing molecules is possible and surface forces are unequally distributed, the condensate will accumulate at places with high binding forces; crystallites will arise which may be useful a probes for surface sites with specific physico-chemical properties. Specific “decoration” with crystallites can be achieved nby exposing membrane fracture faces to water vopour. A device was developed which enables the production of pure water vapour and the controlled variation of its partial pressure in an UHV freeze-fracture apparatus (Fig.1a). Under vaccum (≤ 10-3 Torr), small container filled with copper-sulfate-pentahydrate is heated with a heating coil, with the temperature controlled by means of a thermocouple. The water of hydration thereby released enters a storage vessel.

Physico-Chemical Properties of Recombinant Desulphatohirudin

1990 ◽  
Vol 63 (03) ◽  
pp. 499-504 ◽  
Author(s):  
A Electricwala ◽  
L Irons ◽  
R Wait ◽  
R J G Carr ◽  
R J Ling ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Gel Filtration ◽  
Chemical Properties ◽  
Alpha Helix ◽  
Apparent Molecular Weight ◽  
Correlation Spectroscopy ◽  
Nmr Studies ◽  
Recombinant Hirudin ◽  
Physico Chemical ◽  
Recombinant Molecule

SummaryPhysico-chemical properties of recombinant desulphatohirudin expressed in yeast (CIBA GEIGY code No. CGP 39393) were reinvestigated. As previously reported for natural hirudin, the recombinant molecule exhibited abnormal behaviour by gel filtration with an apparent molecular weight greater than that based on the primary structure. However, molecular weight estimation by SDS gel electrophoresis, FAB-mass spectrometry and Photon Correlation Spectroscopy were in agreement with the theoretical molecular weight, with little suggestion of dimer or aggregate formation. Circular dichroism studies of the recombinant molecule show similar spectra at different pH values but are markedly different from that reported by Konno et al. (13) for a natural hirudin-variant. Our CD studies indicate the presence of about 60% beta sheet and the absence of alpha helix in the secondary structure of recombinant hirudin, in agreement with the conformation determined by NMR studies (17)

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