Quality by Design for Optimizing a Novel Liposomal Jojoba Oil-Based Emulgel to Ameliorate the Anti-Inflammatory Effect of Brucine

One of the recent advancements in research is the application of natural products in developing newly effective formulations that have few drawbacks and that boost therapeutic effects. The goal of the current exploration is to investigate the effect of jojoba oil in augmenting the anti-inflammatory effect of Brucine natural alkaloid. This is first development of a formulation that applies Brucine and jojoba oil int a PEGylated liposomal emulgel proposed for topical application. Initially, various PEGylated Brucine liposomal formulations were fabricated using a thin-film hydration method. (22) Factorial design was assembled using two factors (egg Phosphatidylcholine and cholesterol concentrations) and three responses (particle size, encapsulation efficiency and in vitro release). The optimized formula was incorporated within jojoba oil emulgel. The PEGylated liposomal emulgel was inspected for its characteristics, in vitro, ex vivo and anti-inflammatory behaviors. Liposomal emulgel showed a pH of 6.63, a spreadability of 48.8 mm and a viscosity of 9310 cP. As much as 40.57% of Brucine was released after 6 h, and drug permeability exhibited a flux of 0.47 µg/cm2·h. Lastly, % of inflammation was lowered to 47.7, which was significant effect compared to other formulations. In conclusion, the anti-inflammatory influence of jojoba oil and Brucine was confirmed, supporting their integration into liposomal emulgel as a potential nanocarrier.

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A Novel Sustained Anti-Inflammatory Effect of Atorvastatin—Calcium PLGA Nanoparticles: In Vitro Optimization and In Vivo Evaluation

Pharmaceutics ◽

10.3390/pharmaceutics13101658 ◽

2021 ◽

Vol 13 (10) ◽

pp. 1658

Author(s):

Dalia H. Abdelkader ◽

Ahmed Kh. Abosalha ◽

Mohamed A. Khattab ◽

Basmah N. Aldosari ◽

Alanood S. Almurshedi

Keyword(s):

Particle Size ◽

Zeta Potential ◽

In Vitro Release ◽

In Vivo Evaluation ◽

Water Emulsion ◽

Atorvastatin Calcium ◽

Anti Inflammatory ◽

Inflammatory Effect

Atorvastatin Calcium (At-Ca) has pleiotropic effect as anti-inflammatory drug beside its main antihyperlipidemic action. Our study was conducted to modulate the anti-inflammatory effect of At-Ca to be efficiently sustained for longer time. Single oil-water emulsion solvent evaporation technique was used to fabricate At-Ca into polymeric nanoparticles (NPs). In vitro optimization survey was performed on Poly(lactide-co-glycolide) (PLGA) loaded with At-Ca regrading to particle size, polydispersity index (PDI), zeta potential, percent entrapment efficiency (% EE), surface morphology and in vitro release pattern. In vitro drug-polymers interactions were fully scanned using Fourier-Transform Infrared Spectroscopy (FTIR) and Differential Scanning calorimetry (DSC) proving that the method of fabrication is an optimal strategy maintaining the drug structure with no interaction with polymeric matrix. The optimized formula with particle size (248.2 ± 15.13 nm), PDI (0.126 ± 0.048), zeta potential (−12.41 ± 4.80 mV), % EE (87.63 ± 3.21%), initial burst (39.78 ± 6.74%) and percent cumulative release (83.63 ± 3.71%) was orally administered in Male Sprague–Dawley rats to study the sustained anti-inflammatory effect of At-Ca PLGA NPs after carrageenan induced inflammation. In vivo results demonstrate that AT-Ca NPs has a sustained effect extending for approximately three days. Additionally, the histological examination revealed that the epidermal/dermal layers restore their typical normal cellular alignment with healthy architecture.

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Sorbaria kirilowii Ethanol Extract Exerts Anti-Inflammatory Effects In Vitro and In Vivo by Targeting Src/Nuclear Factor (NF)-κB

Biomolecules ◽

10.3390/biom10050741 ◽

2020 ◽

Vol 10 (5) ◽

pp. 741 ◽

Cited By ~ 1

Author(s):

Jiwon Jang ◽

Jong Sub Lee ◽

Young-Jin Jang ◽

Eui Su Choung ◽

Wan Yi Li ◽

...

Keyword(s):

Signaling Pathways ◽

Ex Vivo ◽

Ethanol Extract ◽

Inflammatory Activity ◽

No Production ◽

Nuclear Factor ◽

Anti Inflammatory ◽

Inflammatory Effect

Inflammation is a fundamental process for defending against foreign antigens that involves various transcriptional regulatory processes as well as molecular signaling pathways. Despite its protective roles in the human body, the activation of inflammation may also convey various diseases including autoimmune disease and cancer. Sorbaria kirilowii is a plant originating from Asia, with no anti-inflammatory activity reported. In this paper, we discovered an anti-inflammatory effect of S. kirilowii ethanol extract (Sk-EE) both in vivo and in vitro. In vitro effects of Sk-EE were determined with lipopolysaccharide (LPS)-stimulated RAW264.7 cells, while ex vivo analysis was performed using peritoneal macrophages of thioglycollate (TG)-induced mice. Sk-EE significantly reduced the nitric oxide (NO) production of induced macrophages and inhibited the expression of inflammation-related cytokines and the activation of transcription factors. Moreover, treatment with Sk-EE also decreased the activation of proteins involved in nuclear factor (NF)-κB signaling cascade; among them, Src was a prime target of Sk-EE. For in vivo assessment of the anti-inflammatory effect of Sk-EE, HCl/EtOH was given by the oral route to mice for gastritis induction. Sk-EE injection dose-dependently reduced the inflammatory lesion area of the stomach in gastritis-induced mice. Taking these results together, Sk-EE exerts its anti-inflammatory activity by regulating intracellular NF-κB signaling pathways and also shows an authentic effect on reducing gastric inflammation.

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Comparison of the Therapeutic Effects of Gold Nanoclusters and Gold Nanoparticles on Rheumatoid Arthritis

Journal of Biomedical Nanotechnology ◽

10.1166/jbn.2019.2848 ◽

2019 ◽

Vol 15 (11) ◽

pp. 2281-2290 ◽

Cited By ~ 3

Author(s):

Yao Zhao ◽

Zhesheng He ◽

Ruoping Wang ◽

Pengju Cai ◽

Xiangchun Zhang ◽

...

Keyword(s):

Rheumatoid Arthritis ◽

Au Nanoparticles ◽

Type Ii Collagen ◽

Therapeutic Effects ◽

Type Ii ◽

Au Clusters ◽

Anti Inflammatory ◽

Inflammatory Effect

Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by synovial inflammation and progressive cartilage and bone damage. In our previous studies, we found that Au clusters using glutathione as a template (GACs) produced profound anti-inflammatory effects in vitro on lipopolysaccharide (LPS)-induced inflammation in mouse macrophage RAW 264.7 cells and type II collagen-induced rat RA in vivo. In this study, we examined whether the template for Au clusters synthesis has an effect on its anti-inflammatory effect and whether Au nanoparticles with larger particle diameter produce the same anti-inflammatory effect. We synthesized Au clusters with bovine serum albumin (BSA) as a template (BACs), Au clusters with glutathione (GSH) as a template (GACs), and Au nanoparticles with glutathione as a template (GANs) and compared their anti-inflammatory effects in vitro and in vivo. These three Au nanomaterials can inhibit the production of lipopolysaccharide (LPS)-induced proinflammatory mediators and ameliorate type II collagen-induced rat RA. However, although the three Au nanomaterials produced similar anti-inflammatory effects, the GANs with larger particle sizes were less stable in vivo and accumulated in the peritoneum after intraperitoneal injection, resulting in poor absorption in vivo. The BACs showed relatively high liver accumulation due to the larger molecular weight of the outer shell. Therefore, we believe that the GACs are potential reliable nanodrugs for the treatment of RA.

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In vivo photoprotective and anti-inflammatory effect of hyperforin is associated with high antioxidant activity in vitro and ex vivo

European Journal of Pharmaceutics and Biopharmaceutics ◽

10.1016/j.ejpb.2012.03.002 ◽

2012 ◽

Vol 81 (2) ◽

pp. 346-350 ◽

Cited By ~ 39

Author(s):

Martina C. Meinke ◽

Sabine Schanzer ◽

Stefan F. Haag ◽

Federica Casetti ◽

Marcel L. Müller ◽

...

Keyword(s):

Antioxidant Activity ◽

Ex Vivo ◽

High Antioxidant Activity ◽

Anti Inflammatory ◽

Inflammatory Effect

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Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel

Polymers ◽

10.3390/polym13040577 ◽

2021 ◽

Vol 13 (4) ◽

pp. 577 ◽

Cited By ~ 2

Author(s):

Wafaa E. Soliman ◽

Tamer M. Shehata ◽

Maged E. Mohamed ◽

Nancy S. Younis ◽

Heba S. Elsewedy

Keyword(s):

Ex Vivo ◽

Skin Permeation ◽

In Vitro Release ◽

Aqueous Solubility ◽

Delivery Methods ◽

Anti Cancer ◽

Permeation Studies ◽

Anti Inflammatory

Background: Curcumin (Cur) possesses a variety of beneficial pharmacological properties including antioxidant, antimicrobial, anti-cancer and anti-inflammatory activities. Nevertheless, the low aqueous solubility and subsequent poor bioavailability greatly limits its effectiveness. Besides, the role of myrrh oil as an essential oil in treating inflammatory disorders has been recently demonstrated. The objective of the current investigation is to enhance Cur efficacy via developing Cur nanoemulgel, which helps to improve its solubility and permeability, for transdermal delivery. Methods: The formulated preparations (Cur gel, emulgel and nanoemulgel) were evaluated for their physical appearance, spreadability, viscosity, particle size, in vitro release and ex vivo drug permeation studies. The in vivo anti-inflammatory activity was estimated using the carrageenan-induced rat hind paw edema method. Results: The formulated Cur-loaded preparations exhibited good physical characteristics that were in the acceptable range of transdermal preparations. The release of Cur from gel, emulgel and nanoemulgel after 12 h was 72.17 ± 3.76, 51.93 ± 3.81 and 62.0 ± 3.9%, respectively. Skin permeation of Cur was significantly (p < 0.05) improved when formulated into nanoemulgel since it showed the best steady state transdermal flux (SSTF) value (108.6 ± 3.8 µg/cm2·h) with the highest enhancement ratio (ER) (7.1 ± 0.2). In vivo anti-inflammatory studies proved that Cur-loaded nanoemulgel displayed the lowest percent of swelling (26.6% after 12 h). Conclusions: The obtained data confirmed the potential of the nanoemulgel dosage form and established the synergism of myrrh oil and Cur as an advanced anti-inflammatory drug.

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Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect

Pharmaceutics ◽

10.3390/pharmaceutics13122037 ◽

2021 ◽

Vol 13 (12) ◽

pp. 2037

Author(s):

Ágota Pető ◽

Dóra Kósa ◽

Ádám Haimhoffer ◽

Pálma Fehér ◽

Zoltán Ujhelyi ◽

...

Keyword(s):

Macrophage Activation ◽

In Vitro Release ◽

Antioxidant Effect ◽

Penetration Enhancers ◽

Drug Candidate ◽

Uvb Radiation ◽

Anti Inflammatory ◽

Inflammatory Effect

BGP-15 is a Hungarian-developed drug candidate with numerous beneficial effects. Its potential anti-inflammatory effect is a common assumption, but it has not been investigated in topical formulations yet. The aim of our study was to formulate 10% BGP-15 creams with different penetration enhancers to ensure good drug delivery, improve bioavailability of the drug and investigate the potential anti-inflammatory effect of BGP-15 creams in vivo. Since the exact mechanism of the effect is still unknown, the antioxidant effect (tested with UVB radiation) and the ability of BGP-15 to decrease macrophage activation were evaluated. Biocompatibility investigations were carried out on HaCaT cells to make sure that the formulations and the selected excipients can be safely used. Dosage form studies were also completed with texture analysis and in vitro release with Franz diffusion chamber apparatus. Our results show that the ointments were able to reduce the extent of local inflammation in mice, but the exact mechanism of the effect remains unknown since BGP-15 did not show any antioxidant effect, nor was it able to decrease LPS-induced macrophage activation. Our results support the hypothesis that BGP-15 has a potential anti-inflammatory effect, even if it is topically applied, but the mechanism of the effect remains unclear and requires further pharmacological studies.

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Enhancement of Anti-Inflammatory Activity of Optimized Niosomal Colchicine Loaded into Jojoba Oil-Based Emulgel Using Response Surface Methodology

Gels ◽

10.3390/gels8010016 ◽

2021 ◽

Vol 8 (1) ◽

pp. 16

Author(s):

Heba S. Elsewedy ◽

Nancy S. Younis ◽

Tamer M. Shehata ◽

Maged E. Mohamed ◽

Wafaa E. Soliman

Keyword(s):

Particle Size ◽

Natural Product ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Inflammatory Activity ◽

Jojoba Oil ◽

Paw Edema ◽

Anti Inflammatory ◽

Vitro Release

Recent progression in investigational studies aiming to integrate natural products and plant oils in developing new dosage forms that would provide optimal therapeutic effect. Therefore, the aim of the present exploration was to inspect the influence of jojoba oil in boosting the anti-inflammatory effect of colchicine natural product. To our knowledge, there is no formulation comprising colchicine and jojoba oil together to form a niosomal emulgel preparation anticipated for topical application. Colchicine is a natural product extracted from Colchicum autumnale that has been evidenced to show respectable anti-inflammatory activity. Owing to its drawbacks and low therapeutic index, it was preferable to be formulated into topical dosage form. The current study inspected colchicine transdermal delivery by developing niosomal preparation as a potential nanocarrier included into emulgel prepared with jojoba oil. Box Behnken design was constructed to develop 17 niosomal emulgel formulations. The optimized colchicine niosomal emulgel was evaluated for its physical characteristics and in vitro release studies. The in vivo anti-inflammatory activity was estimated via carrageenan-induced rat hind paw edema method. The developed colchicine niosomal preparation revealed particle size of 220.7 nm with PDI value 0.22, entrapment efficiency 65.3%. The formulation was found to be stable showing no significant difference in particle size and entrapment efficiency up on storage at 4 °C and 25 °C for 3 months. The optimized colchicine niosomal emulgel exhibited a pH value 6.73, viscosity 4598 cP, and spreadability 38.3 mm. In vitro release study of colchicine from niosomal emulgel formulation was around 52.4% over 6 h. Apparently, the proficient anti-inflammatory activity of colchicine niosomal emulgel was confirmed via carrageenan-induced rat hind paw edema test. Overall, the results recommend the combination of niosomal preparation with jojoba oil-based emulgel that might signify a favorable delivery of anti-inflammatory drug such as colchicine.

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STUDY OF ENHANCED ANTI-INFLAMMATORY POTENTIAL OF NIGELLA SATIVA IN TOPICAL NANOFORMULATION

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2018v10i7.22966 ◽

2018 ◽

Vol 10 (7) ◽

pp. 41 ◽

Cited By ~ 3

Author(s):

Faisal Obaid Alotaibi ◽

Gulam Mustafa ◽

Alka Ahuja

Keyword(s):

Zeta Potential ◽

Size Distribution ◽

Therapeutic Potential ◽

Ex Vivo ◽

Nigella Sativa ◽

In Vitro Release ◽

Spherical Shape ◽

Active Constituent ◽

Anti Inflammatory

Objective: Formulate a nanocarrier for enhancing the anti-inflammatory activity of thymoquinone (Tq), a major active constituent of Nigella sativa.Methods: Nanoformulation of Tq was developed by low energy emulsification techniques. NanoTqs were pre-screened by different thermodynamic stability tests, followed by in vitro release, zeta potential, viscosity, the transmittance (%), globule size distribution and ex vivo studies. The morphology of the optimized NanoTq was determined by transmission electron microscopy (TEM) which revealed fairly spherical shape and good correlation with particle size distribution study. The formulation used for assessment of the anti-inflammatory potential and permeability enhancement contained mixture of essential oil of Nigella sativa: Capryol 90 (3:7, 10%, v/v), Tween 80 (21.75%, v/v), PEG 400 (7.25%, v/v) and double distilled water (61%, v/v).Results: The in vitro permeation of Tq from optimized formulations was found extremely significant (p<0.001) in comparison to apiTq. The steady state flux (Jss), the permeability coefficient (Kp) and enhancement ratio (Er) of NanoTq gel was determined and compared with apiTq. The comparative anti-inflammatory effects of the optimized formulations NanoTq, apiTq and DicloGel was assessed on the edema in the carrageenan-induced paw model in Wistar rats. Therapeutic potential of NanoTq was found statistically extremely significant (P<0.0001) compared to apiTq and insignificant comparable with standard DicloGel. Storage stability of NanoTq showed insignificant changes in the zeta potential, droplet size and was free from any physical instability.Conclusion: The optimized nano formulation with a lower dose of Tq showed better anti-inflammatory effects, indicating greater absorption capability through the stratum corneum.

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Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities

Antioxidants ◽

10.3390/antiox9090787 ◽

2020 ◽

Vol 9 (9) ◽

pp. 787 ◽

Cited By ~ 1

Author(s):

María Jesús Pérez de Vega ◽

Silvia Moreno-Fernández ◽

Gloria María Pontes-Quero ◽

María González-Amor ◽

Blanca Vázquez-Lasa ◽

...

Keyword(s):

Ex Vivo ◽

Radical Scavenging Activity ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Antioxidant Compounds ◽

Therapeutic Effects ◽

Protective Effects ◽

Therapeutic Benefits ◽

Anti Inflammatory

Antioxidant compounds, including polyphenols, have therapeutic effects because of their anti-inflammatory, antihypertensive, antithrombotic and antiproliferative properties. They play important roles in protecting the cardiovascular and neurological systems, by having preventive or protective effects against free radicals produced by either normal or pathological metabolism in such systems. For instance, resveratrol, a well-known potent antioxidant, has a counteracting effect on the excess of reactive oxygen species (ROS) and has a number of therapeutic benefits, like anti-inflammatory, anti-cancer and cardioprotective activities. Based on previous work from our group, and on the most frequent OH substitutions of natural polyphenols, we designed two series of synthetically accessible bis-polyhydroxyphenyl derivatives, separated by amide or urea linkers. These compounds exhibit high antioxidant ability (oxygen radical absorbance capacity (ORAC) assay) and interesting radical scavenging activity (RSA) values (2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and α,α-diphenyl-β-picrylhydrazyl (DPPH) tests). Some of the best polyphenols were evaluated in two biological systems, endothelial cells (in vitro) and whole aorta (ex vivo), highly susceptible for the deleterious effects of prooxidants under different inflammatory conditions, showing protection against oxidative stress induced by inflammatory stimuli relevant in cardiovascular diseases, i.e., Angiotensin II and IL-1β. Selected compounds also showed strong in vivo antioxidant properties when evaluated in the model organism Saccharomyces cerevisiae.

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DEVELOPMENT OF SEMISOLID PREPARATIONS CONTAINING EXTRACT OF THAI POLYHERBAL RECIPE FOR ANTI-INFLAMMATORY EFFECT

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i4.33902 ◽

2019 ◽

pp. 345-353

Author(s):

Sirawan Gunsuang ◽

Napaphak Jaipakdee ◽

Pramote Mahakunakorn ◽

Ekapol Limpongsa

Keyword(s):

In Vitro Release ◽

Ethanolic Extract ◽

Raw 264.7 Cells ◽

Total Phenolic ◽

No Production ◽

Dependent Manner ◽

Skin Delivery ◽

Anti Inflammatory ◽

Inflammatory Effect

Objective: The objective was to develop the semisolid preparations containing extract of Thai polyherbal recipe with anti-inflammatory effect. Methods: Polyherbal ethanolic extract was prepared by maceration and determined for phytochemicals and antioxidant activity. Effects of extract on the production of pro-inflammatory mediator-nitric oxide (NO)-were examined in RAW 264.7 cells. Semisolid preparations, balm, and gel, were prepared and evaluated. In vitro release profiles and mechanisms of phenolic compounds, phytochemical markers, from the preparations were investigated. Results: Polyherbal ethanolic extract was dark yellow-green, viscous liquid with the yields of 8.2%. Total phenolic and total flavonoid contents were 121.21±1.60 mg GAE/g and 26.55±1.38 mg QE/g, respectively. Antioxidant assay showed that polyherbal extract can scavenge the radical to a certain extent, with DPPH IC50 of 160.75±3.43 µg/ml and FRAP values of 91.94±4.17 mg FeSO4/g. In vitro anti-inflammatory test revealed that the extract inhibited NO production in a dose-dependent manner, with IC50 of 145.65±3.26 µg/ml. The yellowish-green color, homogenous and suitable for skin application polyherbal balm and gel was obtained. The higher release of phenolics from the gel was observed, with the cumulative release at 8 h of 119.0±4.3 mg GAE, whereas that from the balm was only 39.7±2.0 mg GAE. The phenolic release profile was found to be best fitted with the Higuchi model. Conclusion: The semisolid preparations containing Thai polyherbal recipe extract with anti-inflammatory effect were successfully prepared. The proper semisolid base and compositions are crucial for effective skin delivery as they influence the release rates of phytochemical markers.

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