Formulation, characterization and ex vivo study of curcumin nano-invasomal gel for enhanced transdermal delivery

Kumar, Bhumika; Sahoo, Prabhat K.; Manchanda, Satish

doi:10.1016/j.onano.2022.100058

Cited by 15 publications

(9 citation statements)

References 24 publications

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“…The resulting slope of the plot provided the flux value in μg/cm 2 /h. The results are in agreement with the previous study performed by Kumar et al…”

Section: Resultsmentioning

confidence: 99%

Curcumin Encapsulation in Geranium Oil Microemulsion Elevates Its Antibacterial, Antioxidant, Anti-Inflammatory, and Anticancer Activities

Hassan,

Asghar,

Ullah Khan

et al. 2024

ACS Omega

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One of the major challenges with curcumin is its poor solubility in water, which limits its absorption and bioavailability in the body. This study aimed to develop and characterize stable microemulsions (MEs) as MEs increase the dispersibility of curcumin in water and aid its absorption in the body. Curcumin-loaded MEs were developed with the goal of enhancing topical delivery and its pharmacological activity (antioxidant, antibacterial, anticancer activity, and anti-inflammatory). The pseudoternary phase diagram was constructed to find out the desired microemulsion region. The prepared MEs (ME1− ME5) were evaluated for pH, viscosity, size of the particle, electrical conductivity, zeta potential, and ex vivo permeation of the drug. The optimized ME formulation was selected based on particle size and was further evaluated for biological activity (in vitro/vivo). In vitro cytotoxic effects of formulations were checked on the human liver cancer cell line, HEPG2 (a cell line exhibiting epithelial-like morphology that was isolated from a hepatocellular carcinoma). Geranium oil, Tween 80 (as a surfactant), and propylene glycol (as a cosurfactant) were screened out based on solubility to formulate MEs. The optimized ME formulation (ME5), with a composition of 20:50:30 (geranium oil:Tween 80:propylene glycol), exhibited pH 4.36 ± 0.057, conductivity of 40.06 ± 0.05 μS/cm, viscosity of 165 ± 0.37 mPa•s, and droplet diameter of 199.39 ± 0.017 nm. The ex vivo permeation study demonstrated a significant cumulative amount of curcumin permeated in 24 h and had a flux of 130.91 ± 0.02 μg/cm 2 /h. Antioxidant activity demonstrated that curcuminloaded microemulsion (ME5) exhibited higher scavenging activity (99.27 ± 0.021%) than blank microemulsion (94.67 ± 0.001%). Optimized curcumin-loaded microemulsion (ME5) exhibited zones of inhibition of 25.18 and 28.37 mm against Escherichia coli and Staphylococcus aureus, respectively. Among the cell lines tested, a higher concentration of ME5 showed the greatest cytotoxicity with a % viability of 8.22 ± 1.09%. Evidently, it also revealed significant in vivo anti-inflammatory effects with 93.29 ± 0.030% inhibition by the carrageenan-induced paw edema model (6 h study) and 88.39 ± 0.002% inhibition by the formalin-induced paw edema model (14 day study). In conclusion, microemulsion was safe and effective for effective delivery of curcumin with the potential for antioxidant, antibacterial, cytotoxic, and in vivo anti-inflammatory activities.

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“…The resulting slope of the plot provided the flux value in μg/cm 2 /h. The results are in agreement with the previous study performed by Kumar et al…”

Section: Resultsmentioning

confidence: 99%

Curcumin Encapsulation in Geranium Oil Microemulsion Elevates Its Antibacterial, Antioxidant, Anti-Inflammatory, and Anticancer Activities

Hassan,

Asghar,

Ullah Khan

et al. 2024

ACS Omega

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“…Terpene oil (Citronella oil, B) concentration increases the VS, but it has less effect than soy lecithin. It may be due to the large amount of LZ encapsulated in IVS with terpenes, which leads to an increase in the size of the IVS [ 45 , 46 ]. On increasing the sonication time, the VS of LZIVS decreased due to of breaking of the vesicle.…”

Section: Resultsmentioning

confidence: 99%

“…The spreadability assists in the consistent application of gel to the skin and greatly impacts patient compliance and therapeutic efficacy. An optimum value of spreadability indicates the gel spreads appropriately in less time and stays for a longer time over the skin [ 46 ]. The spreadability of all LZIVSopt gel was determined, and the result is shown in Table 3 .…”

Section: Resultsmentioning

confidence: 99%

Development of Soft Luliconazole Invasomes Gel for Effective Transdermal Delivery: Optimization to In-Vivo Antifungal Activity

Kumari,

Alsaidan,

Mohanty

et al. 2023

Gels

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Luliconazole (LZ) is a good candidate for the treatment of fungal infection topically but has limitations, i.e., poor solubility and poor permeability to skin. Due to these limitations, multiple administrations for a long time are required to treat the inflection. The aim of the present study was to develop the invasomes (IVS) gel of LZ to improve the topical antifungal activity. The IVS was prepared by the thin-film hydration method and optimized by Box-Bhekhen design software. The optimized LZIVS (LZIVSopt) has 139.1 ± 4.32 nm of vesicle size, 88.21 ± 0.82% of entrapment efficiency, 0.301 ± 0.012 of PDI, and 19.5 mV (negative) of zeta potential. Scanning microscopy showed a spherical shape of the vesicle. FTIR spectra showed there is no interaction between the drug and lipid. Thermogram showed that the LZ is encapsulated into the LZIVS matrix. LZIVSopt gel (LZIVSopt-G3) exhibited optimum viscosity (6493 ± 27 cps) and significant spreadability (7.2 g·cm/s). LZIVSopt-G3 showed 2.47-fold higher permeation than pure LZ-gel. LZIVSopt-G3 did not show any edema or swelling in the skin, revealing that the developed formulation is non-irritant. LZIVSopt-G3 exhibited significant inhibition of the fungus infection (C. albicans) in the infected rats. The finding concluded that IVS gel is a good carrier and an attractive approach for the enhancement of topical delivery of LZ to treat the fungal infection.

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“…15 The ability to multiple drug entrapment along with high skin permeability can make these vesicles as a suitable option to create appropriate skin formulations. 16,17 Bupivacaine and buprenorphine are classified as strong local analgesics and opioids, respectively, 18 but due to their physicochemical properties, they do not have suitable conditions for skin penetration. Concomitant use of opioids and local anaesthetics may have a synergistic effect and may also block skin-concentrated opioid receptors and free nerve endings simultaneously.…”

Section: Introductionmentioning

confidence: 99%

“…These vesicles are mainly composed of phospholipids, ethanol and terpenes that give soft and flexible properties 15 . The ability to multiple drug entrapment along with high skin permeability can make these vesicles as a suitable option to create appropriate skin formulations 16,17 . Bupivacaine and buprenorphine are classified as strong local analgesics and opioids, respectively, 18 but due to their physicochemical properties, they do not have suitable conditions for skin penetration.…”

Section: Introductionmentioning

confidence: 99%

Nano‐invasomes for simultaneous topical delivery of buprenorphine and bupivacaine for dermal analgesia

Babaie

Charkhpour

Kouhsoltani

et al. 2023

Experimental Dermatology

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Opioid and local anaesthetic receptors are abundantly concentrated in different layers of the skin. Therefore, simultaneous targeting of these receptors can produce more potent dermal anaesthesia. Herein, we developed lipid‐based nanovesicles for the co‐delivery of buprenorphine and bupivacaine to efficiently target skin‐concentrated pain receptors. Invasomes incorporating two drugs were prepared by ethanol injection method. Subsequently, the size, zeta potential, encapsulation efficiency, morphology, and in‐vitro drug release of vesicles were characterized. Ex‐vivo penetration features of vesicles were then investigated by the franz diffusion cell on the full‐thickness human skin. Wherein, it was demonstrated that invasomes penetrated the skin deeper and delivered bupivacaine more effectively than buprenorphine to the target site. The superiority of invasome penetration was further evidenced by the results of ex‐vivo fluorescent dye tracking. Estimation of in‐vivo pain responses by the tail‐flick test revealed that compared with the liposomal group, the group receiving invasomal formulation and drug‐free invasomal formulation (only containing menthol) displayed increased analgesia in the initial times of 5 and 10 min. Also, no signs of oedema or erythema were observed in the Daze test in any of the rats receiving the invasome formulation. Finally, ex‐vivo and in‐vivo assays demonstrated efficiency in delivering both drugs into deeper layers of skin and exposing them to the located pain receptors, which improves the time of onset and the analgesic effects. Hence, this formulation appears to be a promising candidate for tremendous development in the clinical setting.

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Formulation, characterization and ex vivo study of curcumin nano-invasomal gel for enhanced transdermal delivery

Cited by 15 publications

References 24 publications

Curcumin Encapsulation in Geranium Oil Microemulsion Elevates Its Antibacterial, Antioxidant, Anti-Inflammatory, and Anticancer Activities

Curcumin Encapsulation in Geranium Oil Microemulsion Elevates Its Antibacterial, Antioxidant, Anti-Inflammatory, and Anticancer Activities

Development of Soft Luliconazole Invasomes Gel for Effective Transdermal Delivery: Optimization to In-Vivo Antifungal Activity

Nano‐invasomes for simultaneous topical delivery of buprenorphine and bupivacaine for dermal analgesia

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