Nanoemulgel: A Novel Nano Carrier as a Tool for Topical Drug Delivery

Donthi, Mahipal Reddy; Munnangi, Siva Ram; Krishna, Kowthavarapu Venkata; Saha, Ranendra N.; Singhvi, Gautam; Dubey, Sunil Kumar

doi:10.3390/pharmaceutics15010164

Cited by 57 publications

(34 citation statements)

References 151 publications

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“…Despite this, it also provides high drug loading, better drug diffusion, biocompatibility, and minimized irritancy. 35 The current study reported ketoconazole-loaded NEGs based on clove oil (clove-oil−NEG) and eucalyptus oil (eucalyptusoil−NEG) in the gelling agent carbopol 943 and HPMC for improved therapy against candidiasis. An extensive preformulation study was performed on the API and their physicochemical properties for developing a robust, stable, and effective dosage form.…”

Section: Discussionmentioning

confidence: 99%

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Natural Oils Enhance the Topical Delivery of Ketoconazole by Nanoemulgel for Fungal Infections

Ahmad,

Farheen,

Kukreti

et al. 2023

ACS Omega

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Nanoemulgel (NEG) pharmaceutical formulations are gaining popularity because of their ability to serve both as a nanoemulsion and as a gel. These products are well-known for their ease of use, spreadability, controlled release, and ability to hydrate dry skin. Natural essential oils have been shown to promote the cutaneous permeability of topical formulations, enhancing medication safety and efficacy. Herein, we developed NEG for the enhanced permeation of ketoconazole against candidiasis using clove oil (clove-oil–NEG) or eucalyptus oil (eucalyptus-oil–NEG), using the gelling agents carbopol 943 and hydroxypropyl methylcellulose (HPMC). We tested various excipients to increase the solubility of ketoconazole and formulate a nanoemulsion (NE). We measured the NE droplet particle size, shape, entrapment efficiency, and drug release. Furthermore, the physicochemical properties of the optimized nanoemulsion formulation were characterized by techniques such as Fourier transform infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) analysis. The NEs were loaded into gels to form NEGs. NEGs were characterized for drug content, homogeneity, rheology, spreadability, and antifungal activity against Candida albicans, both in vitro and in vivo. Optimized ketoconazole NEG preparations consisted of either 15% clove oil or 20% eucalyptus oil. Droplet sizes in the optimized NEs were <100 nm, and the polydispersity indexes were 0.24 and 0.26. The percentages of ketoconazole released after 24 h from the clove-oil–NEG and eucalyptus-oil–NEGs were 91 ± 4.5 and 89 ± 7%, respectively. Scanning electron microscopy (SEM) showed that the NEGs had a smooth, uniform, and consistent shape and internal structural organization. The drug contents in the clove-oil–NEG and eucalyptus-oil–NEG were 98.5 ± 2.2 and 98.8 ± 3.4%, respectively. Permeation values of ketoconazole from clove-oil–NEG and eucalyptus-oil–NEG were 117 ± 7 and 108.34 ± 6 μg cm–2, respectively. The ketoconazole NEG formulations also had higher levels of fungal growth inhibition than a marketed formulation. Finally, in vivo studies showed that the NEGs do not irritate the skin. Ketoconazole NEG with either 15% clove oil or 20% eucalyptus oil is stable with better efficacy than ketoconazole alone due to excellent dispersion, drug dissolution, and permeability and thus might be recommended for the effective and safe treatment of candidiasis.

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Section: Discussionmentioning

confidence: 99%

“…Nanoemulgel protects medicament from enzymatic degradation and hydrolysis and improves retention and skin permeation. Despite this, it also provides high drug loading, better drug diffusion, biocompatibility, and minimized irritancy …”

Section: Discussionmentioning

confidence: 99%

Natural Oils Enhance the Topical Delivery of Ketoconazole by Nanoemulgel for Fungal Infections

Ahmad,

Farheen,

Kukreti

et al. 2023

ACS Omega

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“…Bio-polysaccharides or their derivatives and proteins belong to natural gelling agents. For instance, bio-polysaccharides are pectin, carrageenan, alginic acid, and gelatin, whilst xanthan gum, starch, and dextran are derivatives of bio-polysaccharides [ 34 ]. However, various kinds of both semi-synthetic and synthetic gelling agents are widely used in emulgel formulation [ 5 ].…”

Section: Formulation Of Emulgelmentioning

confidence: 99%

Emulgels: Promising Carrier Systems for Food Ingredients and Drugs

Milutinov,

Krstonošić,

Ćirin

et al. 2023

Polymers

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Novel delivery systems for cosmetics, drugs, and food ingredients are of great scientific and industrial interest due to their ability to incorporate and protect active substances, thus improving their selectivity, bioavailability, and efficacy. Emulgels are emerging carrier systems that represent a mixture of emulsion and gel, which are particularly significant for the delivery of hydrophobic substances. However, the proper selection of main constituents determines the stability and efficacy of emulgels. Emulgels are dual-controlled release systems, where the oil phase is utilized as a carrier for hydrophobic substances and it determines the occlusive and sensory properties of the product. The emulsifiers are used to promote emulsification during production and to ensure emulsion stability. The choice of emulsifying agents is based on their capacity to emulsify, their toxicity, and their route of administration. Generally, gelling agents are used to increase the consistency of formulation and improve sensory properties by making these systems thixotropic. The gelling agents also impact the release of active substances from the formulation and stability of the system. Therefore, the aim of this review is to gain new insights into emulgel formulations, including the components selection, methods of preparation, and characterization, which are based on recent advances in research studies.

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“…To address these limitations, an emulsion-loaded gel can be used to incorporate and deliver a hydrophobic therapeutic moiety via a topical route. Emulgels are dosage forms produced by combining emulsions and gels, possess high penetration capacity, elegance after application, and can easily be wiped off from the skin [ 23 ]. Emulgels for dermatological use have several advantages, including having thixotropic behavior, acting as an emollient, having a longer shelf life, high drug loading capacity, exhibiting controlled release, and improving stability [ 24 , 25 , 26 ].…”

Section: Introductionmentioning

confidence: 99%

Dasatinib-Loaded Topical Nano-Emulgel for Rheumatoid Arthritis: Formulation Design and Optimization by QbD, In Vitro, Ex Vivo, and In Vivo Evaluation

et al. 2023

Self Cite

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The current study aimed to develop a topical emulgel of dasatinib (DTB) for rheumatoid arthritis (RA) treatment to reduce systemic side effects. The quality by design (QbD) approach was employed to optimize DTB-loaded nano-emulgel using a central composite design (CCD). Emulgel was prepared using the hot emulsification method, and then the particle size (PS) was reduced using the homogenization technique. The PS and % entrapment efficiency (% EE) were found to be 172.53 ± 3.33 nm (0.160 ± 0.014 PDI) and 95.11 ± 0.16%, respectively. The nano-emulsion (CF018 emulsion) in vitro drug release profile showed sustained release (SR) up to 24 h. MTT assay results from an in vitro cell line study revealed that formulation excipients had no effect, whereas emulgel showed a high degree of internalization. Furthermore, emulgel treatment significantly reduced LPS-induced TNF-α production in RAW 264.7 cells. The spherical shape was depicted in FESEM images of optimized nano-emulgel (CF018 emulgel) formulation. Ex vivo skin permeation was significantly increased when compared to the free drug-loaded gel (FDG). In vivo data revealed that the optimized CF018 emulgel is a non-irritant and is safe. In terms of paw swelling, the FCA-induced arthritis model demonstrated that the CF018 emulgel reduced paw swelling percentage compared to adjuvant-induced arthritis (AIA) control group. Following clinical testing in the near future, the designed preparation could be a viable alternative treatment for RA.

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Nanoemulgel: A Novel Nano Carrier as a Tool for Topical Drug Delivery

Cited by 57 publications

References 151 publications

Natural Oils Enhance the Topical Delivery of Ketoconazole by Nanoemulgel for Fungal Infections

Natural Oils Enhance the Topical Delivery of Ketoconazole by Nanoemulgel for Fungal Infections

Emulgels: Promising Carrier Systems for Food Ingredients and Drugs

Dasatinib-Loaded Topical Nano-Emulgel for Rheumatoid Arthritis: Formulation Design and Optimization by QbD, In Vitro, Ex Vivo, and In Vivo Evaluation

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