Development of a novel nanoemulgel formulation containing cumin essential oil as skin permeation enhancer

AbstractEssential oils have been proposed as promising non-toxic transdermal permeation enhancers. Their use is limited because of their low water solubility. The use of nanotechnology-based strategies is one of the ways to overcome this limitation. This study aimed to explore the transdermal permeation enhancing capability of cumin essential oil in nanoemulgel systems containing diclofenac sodium. Cumin essential oil nanoemulsion was produced by high-pressure homogenization technique. The formulation was optimized by changing HLB values in a range of 9.65–16.7 using different surfactant mixtures, namely, Tween 20, Tween 80, and Span 80. Preparations were characterized by polydispersity index, droplet size, and zeta potential. Nanoemulsion with concentrations of 2 and 4% essential oil was incorporated into 0.75% Carbopol gel matrix to make nanoemulgel formulation, and its permeation enhancing effect was performed through Franz diffusion cells. Antinociceptive activities of the formulations were measured in thermal (tail-flick) and chemical (formalin) models of nociception in mice. Characterization exhibited that at HLB value of 9.65, the smallest particle size (82.20 ± 5.82 nm) was formed. By increasing the essential oil percentage in the nanoemulgel from 1 to 2%, the permeation of diclofenac increased from 28.39 ± 1.23 to 34.75 ± 1.07 µg/cm2 at 24 h. The value of permeation from the simple gel (21.18 ± 2.51 µg/cm2) and the marketed product (22.97 ± 1.92 µg/cm2) was lower than the formulations containing essential oil. Nanoemulgel of diclofenac containing essential oil showed stronger antinociceptive effects in formalin and tail-flick tests than simple diclofenac gel and marketed formulation. In conclusion, the study proved that nanoemulgel formulation containing cumin essential oil could be considered as a promising skin enhancer to enhance the therapeutic effect of drugs. Graphical abstract

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Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

The Scientific World JOURNAL ◽

10.1155/2014/127495 ◽

2014 ◽

Vol 2014 ◽

pp. 1-9 ◽

Cited By ~ 17

Author(s):

Saleh A. Al-Suwayeh ◽

Ehab I. Taha ◽

Fahad M. Al-Qahtani ◽

Mahrous O. Ahmed ◽

Mohamed M. Badran

Keyword(s):

Analgesic Activity ◽

Skin Permeation ◽

Tween 80 ◽

Skin Penetration ◽

Penetration Enhancers ◽

Topical Gel ◽

Carbopol Gel ◽

Franz Diffusion Cells ◽

Gel Formulations

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also,in vitroskin permeation of LOR was conducted. The effect of hydroxypropylβ-cyclodextrin (HPβ-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HPβ-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HPβ-CD and may be promising in enhancing permeation.

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Karakteristik Mikroemulsi a-Tokoferol pada Perbandingan Campuran Tiga Surfaktan Nonionik dan Lama Pengadukan

JURNAL REKAYASA DAN MANAJEMEN AGROINDUSTRI ◽

10.24843/jrma.2021.v09.i01.p04 ◽

2021 ◽

Vol 9 (1) ◽

pp. 33

Author(s):

Putu Ayu Sucitawati ◽

Lutfi Suhendra ◽

G. P. Ganda Putra

Keyword(s):

Nonionic Surfactants ◽

Block Design ◽

Tween 80 ◽

Tween 20 ◽

Time Data ◽

Surfactant Mixtures ◽

Mixture Ratio ◽

Randomized Block Design ◽

Hydrophilic Lipophilic Balance ◽

Stirring Time

Microemulsions have thermodynamics and stable kinetics as carriers of ?-tocopherol compounds. This study aimed to know the effect of mixtures ratio of three nonionic surfactants and stiring time on the characteristics of ?-tocopherol microemulsion, as well as to obtain the best stiring time and mixture ratio of three nonionic surfactants to produce ?-tocopherol microemulsion. This experiment used a randomized block design with two factors. The first factor is the ratio of a mixture of three nonionic surfactants with Hydrophilic-Lipophilic Balance (HLB) 14.5. The second factor is stirring time. Data were analyzed using analysis of variance and continued with BNJ test. Test the effectiveness index to determine the best treatment. The results showed that the comparison of three surfactant mixtures, stirring duration and interaction between treatments significantly affected the characteristics of ?-tocopherol microemulsion. Comparison of the mixture of three surfactants Tween 80: Span 80: Tween 20 (v / v%) HLB 14.5 consisting of F2 (89,5 : 5,5 : 5) and 4 minutes stirring time is the best treatment for the characteristics of ?-Tocopherol microemulsion. The best treatment has the characteristics of ?-tocopherol microemulsions namely transparent appearance, stable to centrifugation (4500 rpm), pH (4.5; 5.5 and 6.5) and dilution (1: 9, 1:49 and 1:99) with Turbidity index values ??are below 1 percent. Microemulsion turbidity index values ??before and after centrifugation were 0.19 percent and microemulsion turbidity at pH 4.5 and 1: 9 dilution were 0.11 percent. Keywords: microemulsion, stirring time, surfactan non ionic, ?-Tocoferol

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Development of Mosquito Protective Textiles Using Nanoemulsion of Eucalyptus Globulus and Syzygium Aromaticum Essential Oils Against Malaria Vector, Anopheles Stephensi (Liston)

10.21203/rs.3.rs-446207/v1 ◽

2021 ◽

Author(s):

Zahra Sheikh ◽

Amir Amani ◽

Hamid Reza Basseri ◽

Seyed Hassan MoosaKazemi ◽

Mohammad Mehdi Sedaghat ◽

...

Keyword(s):

Essential Oil ◽

Essential Oils ◽

Malaria Vector ◽

Eucalyptus Globulus ◽

Anopheles Stephensi ◽

Tween 80 ◽

Gas Chromatography Mass Spectrometry ◽

Tween 20 ◽

Syzygium Aromaticum ◽

Nano Emulsion

Abstract Background The aim of current study was to determine the protection efficacy of Eucalyptus globulus and Syzygium aromaticum essential oils nanoemulsions-loaded textiles versus bulk essential oil- treated textiles against the malaria vector, Anopheles stephensi. Methods The components of E. globulus and S. aromaticum essential oils were determined using gas chromatography/mass spectrometry. Then, the nanoemulsions of both essential oils were prepared using a low energy emulsification method. Their stability and droplet sizes were determined, and the repellent efficacy against landings/bites of the starve mosquito females was examined using textile panels of polyester/cotton, impregnated with serial concentrations of the nano-emulsion. Results The main compositions of E. globulus essential oil were 1, 8-cineol (64.58%) and alpha-pinene (10.63%), whereas those of S. aromaticum essential oil were 2-methoxy-3-(2-propenyl) (77.04%) and trans-caryophyllene (11.99%). Transparent oil in water nanoemulsion system consisting of essential oils, Tween-20, Tween-80 and propylene glycol was developed. The median droplet size was 11.2-23.1nm depending on dilution ratio. Protection time of nanoemulsion-loaded textile (285 ± 30 min) was noticeably higher than that of bulk essential oils (< 5 min). Conclusions It was concluded that nanoemulsion of essential oils may be interesting options in control of mosquito-related diseases.

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Skin Permeation of Cacalol, Cacalone and 6-epi-Cacalone Sesquiterpenes from a Nanoemulsion

Natural Product Communications ◽

10.1177/1934578x1200700703 ◽

2012 ◽

Vol 7 (7) ◽

pp. 1934578X1200700 ◽

Cited By ~ 1

Author(s):

María Luisa Garduño-Ramírez ◽

Beatriz Clares ◽

Valeri Domínguez-Villegas ◽

Concepción Peraire ◽

María Adolfina Ruiz ◽

...

Keyword(s):

Natural Products ◽

Skin Permeation ◽

Low Permeability ◽

Transdermal Permeation ◽

Diffusion Cells ◽

Franz Diffusion Cells

The objective of the present study was to investigate the transdermal permeation of cacalol (1) and a mixture of cacalone (2) and 6- epi-cacalone (3) in comparison with diclofenac acid (4) delivered from the same characterized nanoemulsion using Franz diffusion cells (formulae I, II and III). Results show that de Kp, J, Q24, P1 and P2 were higher for the acid diclofenac nanoemulsion than for the natural products nanoemulsions. As for the differences between the formulations I and II, with the natural products, Q24, the quantity extracted from skin and P2 were higher in the mixture of 2 and 3 nanoemulsion compared with the corresponding nanoemulsion of 1. In conclusion, the low permeability of the natural products nanoemulsions in comparison with that of diclofenac acid has the potential for development for drugs with local and systemic applications, respectively.

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Alginate Films Encapsulating Lemongrass Essential Oil as Affected by Spray Calcium Application

Colloids and Interfaces ◽

10.3390/colloids3030058 ◽

2019 ◽

Vol 3 (3) ◽

pp. 58 ◽

Cited By ~ 2

Author(s):

Cofelice ◽

Cuomo ◽

Chiralt

Keyword(s):

Essential Oil ◽

Water Solubility ◽

Film Surface ◽

Tween 80 ◽

Edible Films ◽

Moisture Loss ◽

The Matrix ◽

Food Integrity ◽

Film Stiffness ◽

Lemongrass Essential Oil

The necessity of producing innovative packaging systems has directed the attention of food industries towards the use of biodegradable polymers for developing new films able to protect foods and to extend their shelf-life, with lower environmental impact. In particular, edible films combining hydrophilic and hydrophobic ingredients could retard moisture loss, gas migration and ensure food integrity, reducing the necessity of using synthetic plastics. Alginate-based films obtained from emulsions of lemongrass essential oil (at 0.1% and 0.5%) in aqueous alginate solutions (1%), with Tween 80 as surfactant (0.3%), were obtained by casting and characterized as to microstructure and thermal behavior, as well as tensile, barrier and optical properties. Films were also crosslinked through spraying calcium chloride onto the film surface and the influence of oil emulsification and the crosslinking effect on the final film properties were evaluated. The film microstructure, analyzed through Field Emission Scanning Electron Microscopy (FESEM) revealed discontinuities in films containing essential oil associated with droplet flocculation and coalescence during drying, while calcium diffusion into the matrix was enhanced. The presence of essential oil reduced the film stiffness whereas calcium addition lowered the film’s water solubility, increasing tensile strength and reducing the extensibility coherent with its crosslinking effect.

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AKTIVITAS ANTIBAKTERI DARI DESAIN MIKROEMULSI MINYAK ATSIRI KAYU MANIS

AGROINTEK ◽

10.21107/agrointek.v11i1.2940 ◽

2017 ◽

Vol 11 (1) ◽

pp. 21

Author(s):

Evelyn Djiuardi ◽

Tutun Nugraha

Keyword(s):

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Essential Oil ◽

Carboxymethyl Cellulose ◽

Pathogenic Bacteria ◽

Tween 80 ◽

Tween 20 ◽

Oil In Water ◽

Cinnamon Essential Oil

This research focused on the study of the capability of cinnamon essential oil as antibacterial agent, when it is made as a microemulsion solution. The study occupied further research on specific type, concentration, and amount of emulsifier needed to make the cinnamon essential oil miscible in water without causing destruction in its antibacterial activity. Four different emulsifiers were tested, namely Tween 20, Tween 80, soya lechitin, and carboxymethyl cellulose (CMC) to stabilize the essential oil in water. The emulsifiers were used at 2% w/w, while the essential oil concentrations were varied at 0.5%, 1%, and 1.5%. In this study, the antibacterial activity of the microemulsion solution of cinnamon essential oil was tested against two types of pathogenic bacteria commonly found in foods, namely Staphylococcus aureus and Escherichia coli. Among the four types of emulsifiers, which are used, CMC showed the best results as an emulsifier. The results of this study indicated that microemulsion solution has antibacterial activity best is a combination between the CMC and the essential oil of cinnamon

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Physicochemical Characterization and Antinociceptive Effect of β-cyclodextrin/Lippia pedunculosa Essential Oil in Mice

Current Topics in Medicinal Chemistry ◽

10.2174/1568026618666180607081742 ◽

2018 ◽

Vol 18 (9) ◽

pp. 797-807 ◽

Cited By ~ 1

Author(s):

Paula dos Passos Menezes ◽

Francielly de Oliveira Araujo ◽

Tatianny Araujo Andrade ◽

Igor Araujo Santos Trindade ◽

Heitor Gomes de Araujo-Filho ◽

...

Keyword(s):

Essential Oil ◽

Physicochemical Properties ◽

Water Solubility ◽

Therapeutic Potential ◽

Biological Activities ◽

Antinociceptive Effect ◽

Physicochemical Characterization ◽

Good Tool ◽

Main Challenge ◽

Higher Temperature

Background: Some research studies have shown that Lippia pedunculosa essential oil (EOLP) has interesting biological activities. However, its low water solubility is the main challenge to achieve its therapeutic potential. In this context, Cyclodextrins (CDs) have been widely used in order to overcome this problem due to your capability to improve the physicochemical properties of drugs. Objective: In this perspective, the main goal of this study was to investigate how the improvement of the physicochemical properties of inclusion complexes (EOLP and β-CD) enhance the antinociceptive effect in mice. Methods: To achieve that, we prepared samples by Physical Mixture (PM), Paste Complexation (PC) and Slurry Complexation (SC) methods, followed by their physicochemical characterization. In addition, it was evaluated if the use of β-CD enhances the antinociceptive effect of EOLP in mice. Results: The analysis showed that rotundifolone (72.02%) was the major compound of EOLP and we found out based on DSC results that β-CD protected it from oxidation. In addition, TG techniques demonstrated that the best inclusion methods were PC and SC, due to their greater weight loss (10.8 and 11.6%, respectively) in the second stage (171-312°C), indicating that more complexed oil was released at the higher temperature than oil free. Other characteristics, such as changes in the typical crystalline form, and reduced particle size were observed by SEM and laser diffraction, respectively. The SC was the most effective complexation method, once the presence of rotundifolone was detected by FTIR. Based on that, SC method was used in all mice tests. In this regard, the number of paw licks was reduced for both compounds (all doses), but EOLP was more effective in reducing the nociceptive behavior. Conclusion: Therefore, CDs seem not to be a good tool to enhance the pharmacological properties of EOs rich in peroxide compounds such as rotundifolone.

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Development and Optimization of Sustained Release Moxifloxacin Hydrochloride Loaded Nanoemulsion for Ophthalmic Drug Delivery: A 32 Factorial Design Approach

Micro and Nanosystems ◽

10.2174/1876402912999200826111031 ◽

2020 ◽

Vol 12 ◽

Author(s):

Sagar R. Pardeshi ◽

Harshal A. Mistari ◽

Rakhi S. Jain ◽

Pankaj R. Pardeshi ◽

Rahul L. Rajput ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Factorial Design ◽

Water Solubility ◽

Tween 80 ◽

Drug Release Profile ◽

Sustained Drug Release ◽

Bacterial Conjunctivitis ◽

Promising Alternative

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.

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Optimization of Thymoquinone-Loaded Self-Nanoemulsion for Management of Indomethacin-Induced Ulcer

Dose-Response ◽

10.1177/15593258211013655 ◽

2021 ◽

Vol 19 (2) ◽

pp. 155932582110136

Author(s):

Mohamed F. Radwan ◽

Mohamed A. El-Moselhy ◽

Walied M. Alarif ◽

Mohamed Orif ◽

Nabil K. Alruwaili ◽

...

Keyword(s):

Water Solubility ◽

Nigella Sativa ◽

Tween 80 ◽

Gastric Ulcers ◽

Major Constituent ◽

Globule Size ◽

Polyethylene Glycol 200 ◽

Experimental Values ◽

Nigella Sativa Seed ◽

Strong Agreement

To improve the water solubility of thymoquinone (TQ), a major constituent of Nigella sativa seed oil, a TQ-loaded self-nanoemulsifying drug delivery system (SNEDDS) was prepared. The SNEDDS formulation was optimized using almond oil (AO) (Oil; X1), tween 80 (surfactant; X2) and polyethylene glycol 200 (PEG 200) (cosurfactant; X3) compounds as independent variables. The results showed that the globule size ranged from 65 to 320 nm. In addition, a strong agreement was reached between the system estimation and the experimental values of globule size. To evaluate the gastroprotective effect of optimized TQ-loaded SNEDDS against indomethacin (Indo.)-induced gastric ulcers in comparison with non-emulsified TQ, the ulcer index and histopathological changes were estimated. Optimized TQ-loaded SNEDDS showed improved gastroprotective activity against Indo.-induced ulcers relative to the non-emulsified TQ. In addition, the gastroprotective index was improved by 2-fold in TQ-loaded SNEDDS as compared to non-emulsified TQ. This is attributed to the strong antioxidant and the cytoprotective activities of the TQ. These results demonstrate enhancement of the efficacy of TQ through the optimized SNEDDS.

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