scholarly journals Preparation of Ophthalmic Microemulsions Containing Lithuanian Royal Jelly and Their Biopharmaceutical Evaluation

Processes ◽  
2021 ◽  
Vol 9 (4) ◽  
pp. 616
Author(s):  
Kristina Perminaite Perminaite ◽  
Mindaugas Marksa ◽  
Liudas Ivanauskas ◽  
Kristina Ramanauskiene
Keyword(s):  
Cell Culture ◽  
Royal Jelly ◽  
Biological Activities ◽  
In Vitro Release ◽  
Physicochemical Characteristics ◽  
In Vitro Tests ◽  
Water Type ◽  
Decenoic Acid ◽  
Ophthalmic Delivery

Royal jelly is a natural substance secreted by worker honeybees that possesses antioxidant, anti-inflammatory, and other biological activities. The purpose of this study was to formulate microemulsions with incorporated Lithuanian royal jelly for possible ophthalmic delivery and to evaluate the quality of the microemulsions in vitro. The oil in water type microemulsions were prepared by the oil titration method, incorporating royal jelly, surfactant, co-surfactant, oil, and water. Physicochemical characteristics of the microemulsions and the quantity of 10-hydroxy-2-decenoic acid released in vitro were assessed. The in vitro assessment of prepared microemulsions formulations was performed with the Statens Seruminstitut rabbit cornea (SIRC) cell culture model. The results revealed that the droplet size of all microemulsion formulations was 67.88–124.2 nm and the polydispersity index was lower than 0.180. In the in vitro release study, the release of 10-hydroxy-2-decenoic acid depended on the amount of royal jelly incorporated and on the ratio of surfactant and co-surfactant in formulations. The in vitro tests with the SIRC cell culture line have shown that all formulations were found non-irritating.

scholarly journals Formulation of Ocular In Situ Gels with Lithuanian Royal Jelly and Their Biopharmaceutical Evaluation In Vitro

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3552
Author(s):  
Kristina Perminaite ◽  
Mindaugas Marksa ◽  
Monika Stančiauskaitė ◽  
Tadas Juknius ◽  
Aidas Grigonis ◽  
...  
Keyword(s):  
Cell Culture ◽  
Refractive Index ◽  
Cell Viability ◽  
Royal Jelly ◽  
Biological Activities ◽  
Pharmaceutical Formulations ◽  
Exposure Test ◽  
Cell Culture Line

Royal jelly is a natural substance produced by worker bees that possesses a variety of biological activities, including antioxidant, anti-inflammatory, antibacterial, and protective. Although fresh royal jelly is kept at low temperatures, to increase its stability, it needs to be incorporated into pharmaceutical formulations, such as in situ gels. The aim of this study was to formulate in situ ocular gels containing Lithuanian royal jelly for topical corneal use in order to increase the retention time of the formulation on the ocular surface and bioavailability. Gels were evaluated for physicochemical characteristics (pH, rheological properties, refractive index) and in vitro drug release measuring the amount of 10-hydroxy-2-decenoic acid (10-HDA). An ocular irritation test and cell viability tests were performed using the SIRC (Statens Seruminstitut Rabbit Cornea) cell culture line. Results indicated that all the in situ gels were within an acceptable pH and refractive index range close to corneal properties. Rheology studies have shown that the gelation temperature varies between 25 and 32 °C, depending on the amount of poloxamers. The release studies have shown that the release of 10-HDA from in situ gels is more sustained than royal jelly suspension. All gel formulations were non-irritant according to the short-time exposure test (STE) using the SIRC cell culture line, and long-term cell viability studies indicated that the formulations used in small concentrations did not induce cell death. Prepared in situ gels containing royal jelly have potential for ocular drug delivery, and they may improve the bioavailability, stability of royal jelly, and formation of non-irritant ocular formulations.

scholarly journals Polymeric Nanoparticles of Pistacia lentiscus var. chia Essential Oil for Cutaneous Applications

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 353
Author(s):  
Ilianna Vrouvaki ◽  
Eleni Koutra ◽  
Michael Kornaros ◽  
Konstantinos Avgoustakis ◽  
Fotini N. Lamari ◽  
...  
Keyword(s):  
Essential Oil ◽  
Polymeric Nanoparticles ◽  
In Vitro Release ◽  
Physicochemical Characteristics ◽  
Poly Lactic Acid ◽  
Poly Vinyl Alcohol ◽  
Pistacia Lentiscus ◽  
Shell Material ◽  
Sem Images

Polymeric nanoparticles (NPs) encapsulating Pistacia lentiscus L. var. chia essential oil (EO) were prepared by a solvent evaporation method, in order to obtain a novel carrier for administration on the skin. The specific EO exhibits antimicrobial and anti-inflammatory properties thus stimulating considerable interest as a novel agent for the treatment of minor skin inflammations. The incorporation into nanoparticles could overcome the administration limitations that inserts the nature of the EO. Nanoparticles were prepared, utilizing poly(lactic acid) (PLA) as shell material, due to its biocompatibility and biodegradability, while the influence of surfactant type on NPs properties was examined. Two surfactants were selected, namely poly(vinyl alcohol) (PVA) and lecithin (LEC) and NPs’ physicochemical characteristics i.e. size, polydispersity index (PdI) and ζ-potential were determined, not indicating significant differences (p > 0.05) between PLA/PVA-NPs (239.9 nm, 0.081, -29.1 mV) and PLA/LEC-NPs (286.1 nm, 0.167, −34.5 mV). However, encapsulation efficiency (%EE) measured by GC-MS, was clearly higher for PLA/PVA-NPs than PLA/LEC-NPs (37.45% vs. 9.15%, respectively). Moreover PLA/PVA-NPs remained stable over a period of 60 days. The in vitro release study indicated gradual release of the EO from PLA/PVA-NPs and more immediate from PLA/LEC-NPs. The above findings, in addition to the SEM images of the particles propose a potential structure of nanocapsules for PLA/PVA-NPs, where shell material is mainly consisted of PLA, enclosing the EO in the core. However, this does not seem to be the case for PLA/LEC-NPs, as the results indicated low EO content, rapid release and a considerable percentage of humidity detected by SEM. Furthermore, the Minimum Inhibitory Concentration (MIC) of the EO was determined against Escherichia coli and Bacillus subtilis, while NPs, however did not exhibit considerable activity in the concentration range applied. In conclusion, the surfactant selection may modify the release of EO incorporated in NPs for topical application allowing its action without interfering to the physiological skin microbiota.

scholarly journals Wound Healing Activity of the Essential Oil of Bursera morelensis, in Mice

Molecules ◽  
2020 ◽  
Vol 25 (8) ◽  
pp. 1795
Author(s):  
Judith Salas-Oropeza ◽  
Manuel Jimenez-Estrada ◽  
Armando Perez-Torres ◽  
Andres Eliu Castell-Rodriguez ◽  
Rodolfo Becerril-Millan ◽  
...  
Keyword(s):  
Wound Healing ◽  
Essential Oil ◽  
Cell Viability ◽  
Murine Model ◽  
Biological Activities ◽  
Healing Process ◽  
In Vitro Tests ◽  
Wound Healing Process ◽  
Fibroblast Migration

Bursera morelensis is used in Mexican folk medicine to treat wounds on the skin. It is an endemic tree known as “aceitillo”, and the antibacterial and antifungal activity of its essential oil has been verified; it also acts as an anti-inflammatory. All of these reported biological activities make the essential oil of B. morelensis a candidate to accelerate the wound-healing process. The objective was to determine the wound-healing properties of B. morelensis’ essential oil on a murine model. The essential oil was obtained by hydro-distillation, and the chemical analysis was performed by gas chromatography-mass spectrometry (GC-MS). In the murine model, wound-healing efficacy (WHE) and wound contraction (WC) were evaluated. Cytotoxic activity was evaluated in vitro using peritoneal macrophages from BALB/c mice. The results showed that 18 terpenoid-type compounds were identified in the essential oil. The essential oil had remarkable WHE regardless of the dose and accelerated WC and was not cytotoxic. In vitro tests with fibroblasts showed that cell viability was dose-dependent; by adding 1 mg/mL of essential oil (EO) to the culture medium, cell viability decreased below 80%, while, at doses of 0.1 and 0.01 mg/mL, it remained around 90%; thus, EO did not intervene in fibroblast proliferation, but it did influence fibroblast migration when wound-like was done in monolayer cultures. The results of this study demonstrated that the essential oil was a pro-wound-healing agent because it had good healing effectiveness with scars with good tensile strength and accelerated repair. The probable mechanism of action of the EO of B. morelensis, during the healing process, is the promotion of the migration of fibroblasts to the site of the wound, making them active in the production of collagen and promoting the remodeling of this collagen.

Physicochemical characteristics and in vitro release from oil-based vehicles of peptidomimetics: parenteral depots for intra-articular administration

2010 ◽  
Vol 37 (1) ◽  
pp. 62-71 ◽  
Author(s):  
Brian Thoning Pedersen ◽  
Jesper Østergaard ◽  
Susan Weng Larsen ◽  
Claus Cornett ◽  
Michael Ankersen ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Physicochemical Characteristics ◽  
Vitro Release

STUDIES ON THE IN VITRO ANTITUMOR ACTIVITY OF FATTY ACIDS: II. SATURATED DICARBOXYLIC ACIDS

1960 ◽  
Vol 38 (6) ◽  
pp. 597-603 ◽  
Author(s):  
Joseph F. Morgan ◽  
Susan Tolnai ◽  
Gordon F. Townsend
Keyword(s):  
Fatty Acids ◽  
Antitumor Activity ◽  
Royal Jelly ◽  
Dicarboxylic Acids ◽  
Ehrlich Carcinoma ◽  
Decenoic Acid ◽  
Fatty Acid Chain ◽  
Transplantable Leukemia ◽  
Akr Mice

Previous studies, which showed that 10-hydroxy-2-decenoic acid from royal jelly possessed in vitro antitumor activity, have been extended to saturated dicarboxylic fatty acids. Seven of eight compounds tested in a series of chain length from C3 to C10 completely prevented the development of the ascites forms of the 6C3HED lymphosarcoma, the Ehrlich carcinoma, and the TA3 mammary carcinoma, as well as the transplantable leukemia of AKR mice. This in vitro antitumor activity could be demonstrated only at pH values below 5.0 and required admixture of the tumor cells and test compounds prior to inoculation of the mice. In general, the antitumor activity of the saturated dicarboxylic acids was found to increase progressively with increasing length of the fatty acid chain.

scholarly journals Enhanced Treatment Effects of Tilmicosin Against Staphylococcus aureus Cow Mastitis by Self-Assembly Sodium Alginate-Chitosan Nanogel

Pharmaceutics ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 524 ◽  
Author(s):  
Kaixiang Zhou ◽  
Xiaofang Wang ◽  
Dongmei Chen ◽  
Yuanyuan Yuan ◽  
Shuge Wang ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Self Assembly ◽  
In Vitro Release ◽  
Physicochemical Characteristics ◽  
The Novel ◽  
In Situ Hydrogel ◽  
Treatment Dosage ◽  
Normal Dosage

The Staphylococcus aureus (S. aureus) cow mastitis causes great losses to the cow industry. In order to improve the treatment effect of tilmicosin against cow mastitis, the combination of solid lipid nanoparticle (SLN) technology with in situ hydrogel technology was used to prepare the self-assembly tilmicosin nanogel (TIL-nanogel). The physicochemical characteristics, in vitro release, antibacterial activity and in vivo treatment efficacy of TIL-SLNs and TIL-nanogel were studied, respectively. The results showed the loading capacity (LC), encapsulation efficiency (EE), size, zeta potential and poly dispersion index (PDI) of TIL-nanogel were 23.33 ± 0.77%, 67.89 ± 3.01%, 431.57 ± 12.87 nm, 8.3 ± 0.06 mv and, 0.424 ± 0.032, respectively. The TIL-nanogel showed stronger sustained release in vitro than TIL-SLNs and commercial injection. The cure rate of half dosage and normal dosage of TIL-nanogel was 58.3% and 75.0%, which was higher than that of commercial injection (50.0%) at normal dosage. The results suggest that the treatment dosage of tilmicosin for cow mastitis could be reduced by TIL-nanogel. The novel TIL-nanogel will be beneficial by decreasing the usage of tilmicosin and the treatment costs of cow mastitis.

scholarly journals Botanical and Genetic Identification Followed by Investigation of Chemical Composition and Biological Activities on the Scabiosa atropurpurea L. Stem from Tunisian Flora

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5032
Author(s):  
Soukaina Hrichi ◽  
Raja Chaabane-Banaoues ◽  
Sihem Bayar ◽  
Guido Flamini ◽  
Yassine Oulad El Majdoub ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Atmospheric Pressure Chemical Ionization ◽  
Biological Activities ◽  
Biologically Active ◽  
Genetic Identification ◽  
In Vitro Tests ◽  
Ionization Mass ◽  
Allelopathic Potential ◽  
Bioactive Agents

Scarce information about the phenolic composition of Scabiosa atropurpurea L. is available, and no carotenoid compounds have been reported thus far. In this study the phenolic and carotenoid composition of this plant was both investigated and associated bioactivities were evaluated. Aiming to obtain extracts and volatile fractions of known medicinal plants to valorize them in the pharmaceutical or food industries, two techniques of extraction and five solvents were used to determine the biologically active compounds. Gas chromatography coupled to flame ionization and mass spectrometry and liquid chromatography coupled to photodiode array and atmospheric pressure chemical ionization/electrospray ionization mass spectrometry highlighted the presence of 15 volatiles, 19 phenolics, and 24 natural pigments in Scabiosa atropurpurea L. stem samples; among them, the most abundant were 1,8-cineole, chlorogenic acid, cynaroside, and lutein. Bioactivity was assessed by a set of in vitro tests checking for antioxidant, antibacterial, antifungal, and allelopathic (against Brassica oleracea L. and Lens culinaris Medik) effects. Scabiosa atropurpurea L. stem extracts presented a considerable antioxidant, antibacterial, and allelopathic potential, with less antifungal effectiveness. These results indicate that the volatile fractions and extracts from S. atropurpurea L. stem could be considered as a good source of bioactive agents, with possible applications in food-related, agriculture, and pharmaceutical fields. Genetic investigations showed 97% of similarity with Scabiosa tschiliensis, also called Japanese Scabiosa.

Hypotensive effects of the triterpene oleanolic acid for cardiovascular prevention

2020 ◽  
Vol 13 ◽  
Author(s):  
A. Sureda ◽  
M. Monserrat-Mesquida ◽  
S. Pinya ◽  
P. Ferriol ◽  
S. Tejada
Keyword(s):  
Blood Pressure ◽  
Oleanolic Acid ◽  
Ex Vivo ◽  
Biological Activities ◽  
Cardiovascular Prevention ◽  
In Vivo Studies ◽  
Antihypertensive Activity ◽  
In Vitro Tests

Background:: Hypertension is a high prevalent chronic disease worldwide and a major cardiovascular risk factor. Oleanolic acid (3β-hydroxy-olea-12-en-28-oic acid) is a wide distributed bioactive pentacyclic triterpenoid with diverse biological activities such as anti-inflammatory, hepaprotective anti-diabetic or anti-hypertensive. Objective:: The aim of this study was to review and highlight the available data about antihypertensive activity of oleanolic acid and the described mechanisms of action. Method:: Extensive searches were made in the available literature on oleanolic acid and the data investigating its antihypertensive effects were analysed. Results:: Most of research has been performed on animal models of hypertension, ex vivo studies with aortic ring and some in vitro tests with cell cultures, whereas clinical trials are still lacking. Treatment of hypertensive animals with oleanolic acid significantly ameliorated the rise in the systolic blood pressure. In addition, the hypotensive effects of oleanolic acid are also related to a potent diuretic-natriuretic activity and nephroprotection. In vitro studies have characterized the participation of various signalling pathways that modulate the release of vasodilation mediators. Conclusion:: In vitro and in vivo studies suggest that oleanolic acid effectively reduce blood pressure and could be an interesting co-adjuvant to conventional treatment of hypertension.

Curcumin-loaded niosomes downregulate mRNA expression of pro-inflammatory markers involved in asthma: an in vitro study

Nanomedicine ◽  
2020 ◽  
Vol 15 (30) ◽  
pp. 2955-2970
Author(s):  
Jin-Ying Wong ◽  
Zhao Yin Ng ◽  
Meenu Mehta ◽  
Shakti D Shukla ◽  
Jithendra Panneerselvam ◽  
...  
Keyword(s):  
Mrna Expression ◽  
Inflammatory Markers ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
In Vitro Study ◽  
Physicochemical Characteristics ◽  
Vitro Study ◽  
Tnf Α ◽  
Vitro Release

Aim: In this study, curcumin was encapsulated in niosomes (Nio-Curc) to increase its effectiveness for the treatment of asthma. Materials & methods: The formulation underwent various physicochemical characterization experiments, an in vitro release study, molecular simulations and was evaluated for in vitro anti-inflammatory activity. Results: Results showed that Nio-Curc had a mean particle size of 284.93 ± 14.27 nm, zeta potential of -46.93 and encapsulation efficacy of 99.62%, which demonstrates optimized physicochemical characteristics. Curcumin release in vitro could be sustained for up to 24 h. Additionally, Nio-Curc effectively reduced mRNA transcript expression of pro-inflammatory markers; IL-6, IL-8, IL-1β and TNF-α in immortalized human airway basal cell line (BCi-NS1.1). Conclusion: In this study, we have demonstrated that Nio-Curc mitigated the mRNA expression of pro-inflammatory markers in an in vitro study, which could be applied to treatment of asthma with further studies.

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