Topical nanostructured lipid carrier gel of quercetin and resveratrol: Formulation, optimization, in vitro and ex vivo study for the treatment of skin cancer

Imran, Mohammad; Iqubal, Mohammad Kashif; Imtiyaz, Khalid; Saleem, Sadaf; Mittal, Saurabh; Rizvi, M Moshahid Alam; Ali, Javed; Baboota, Sanjula

doi:10.1016/j.ijpharm.2020.119705

Cited by 134 publications

(57 citation statements)

References 58 publications

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“…For example, previous studies have found that the combination of quercetin with ionizing radiation showed a greater response against colon cancer stem cells. In addition, the combination of quercetin with resveratrol in a dermal gel favored penetration into deeper layers of the skin and thus can serve as a promising component to be used in formulations for the treatment of skin cancer [ 76 , 77 ]. Other results showed that quercetin exhibits inhibitory activity against the growth of metastatic ovarian cancer cells [ 78 ].…”

Section: Resultsmentioning

confidence: 99%

UHPLC-MS Chemical Fingerprinting and Antioxidant, Antiproliferative, and Enzyme Inhibition Potential of Gaultheria pumila Berries

Fernández-Galleguillos

Quesada-Romero

Puerta

et al. 2021

Metabolites

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Gaultheria pumila (Ericaceae) (known as Chaura or Mutilla) is a Chilean native small shrub that produces berry fruits consumed by local Mapuche people. In this study, the chemical fingerprinting and antioxidant, enzyme inhibition, and antiproliferative activities of the berries were investigated for the first time. Thirty-six metabolites were identified in the fruits by ultra-high performance liquid chromatography-photodiode array detection, hyphenated with Orbitrap mass spectrometry analysis (UHPLC-DAD-Orbitrap-MS). Metabolites, included anthocyanins, phenolic acids, flavonoids, iridoids, diterpenes, and fatty acids. Moderate inhibitory activities against acetylcholinesterase (7.7 ± 0.3 µg/mL), butyrylcholinesterase (34.5 ± 0.5 µg/mL), and tyrosinase (3.3 ± 0.2 µg/mL) enzymes were found. Moreover, selected major compounds were subjected to docking assays in light of their experimental inhibition. Results indicated that hydrogen bonding, π–π interaction, and a salt bridge interaction contributed significantly. Gaultheria pumila berries showed a total phenolic content of 189.2 ± 0.2 mg of gallic acid equivalents/g, total flavonoid content of 51.8 ± 0.1 mg quercetin equivalents/g, and total anthocyanin content of 47.3 ± 0.2 mg of cianydin-3-glucoside equivalents/g. Antioxidant activity was assessed using DPPH (92.8 ± 0.1 µg/mL), FRAP (134.1 ± 0.1 μmol Trolox equivalents/g), and ORAC (4251.6 ± 16.9 μmol Trolox equivalents/g) assays. Conversely, Gaultheria pumila showed a scarce antiproliferative potential against several solid human cancer cells. Our findings suggest that Gaultheria pumila berries have several bioactive metabolites with inhibitory effects against acetylcholinesterase, butyrylcholinesterase, and tyrosinase, and have the potential for use in food supplements.

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Section: Resultsmentioning

confidence: 99%

UHPLC-MS Chemical Fingerprinting and Antioxidant, Antiproliferative, and Enzyme Inhibition Potential of Gaultheria pumila Berries

Fernández-Galleguillos

Quesada-Romero

Puerta

et al. 2021

Metabolites

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“…In contrast, the SO-to-Compritol ratio and Labrasol concentration exhibited a negative impact on particle size. This meant that the size of the particles of the nanoformulations was decreased with the increased concentration of independent factors B and C. The reasons behind this phenomenon were found to be a better affinity of MZ toward these factors and the emulsification characteristics of Labrasol, which minimized the particle size and increased the stability of the nanoformulations (Imran et al., 2020 ). Simultaneously, the contour plot and 3D surface plot ( Figure 2 ) exhibited the impact of the independent factors on the particle size of various fabricated NLCs.…”

Section: Resultsmentioning

confidence: 99%

“…To make an optimized NLC-based nanoformulation, an experimental design was utilized as a statistical tool. This approach simplified the exhaustive process of formulation development, and the obtained statistical design and mathematical equations exhibited the effects of different selected variables on the nanoformulations (Imran et al., 2020 ).…”

Section: Introductionmentioning

confidence: 99%

Development, optimization, and evaluation of a nanostructured lipid carrier of sesame oil loaded with miconazole for the treatment of oral candidiasis

et al. 2022

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Candida albicans is the fungus responsible for oral candidiasis, a prevalent disease. The development of antifungal-based delivery systems has always been a major challenge for researchers. This study was designed to develop a nanostructured lipid carrier (NLC) of sesame oil (SO) loaded with miconazole (MZ) that could overcome the solubility problems of MZ and enhance its antifungal activity against oral candidiasis. In the formulation of this study, SO was used as a component of a liquid lipid that showed an improved antifungal effect of MZ. An optimized MZ-loaded NLC of SO (MZ-SO NLC) was used, based on a central composite design-based experimental design; the particle size, dissolution efficiency, and inhibition zone against oral candidiasis were chosen as dependent variables. A software analysis provided an optimized MZ-SO NLC with a particle size of 92 nm, dissolution efficiency of 88%, and inhibition zone of 29 mm. Concurrently, the ex vivo permeation rate of the sheep buccal mucosa was shown to be significantly ( p < .05) higher for MZ-SO NLC (1472 µg/cm 2 ) as compared with a marketed MZ formulation (1215 µg/cm 2 ) and an aqueous MZ suspension (470 µg/cm 2 ). Additionally, an in vivo efficacy study in terms of the ulcer index against C. albicans found a superior result for the optimized MZ-SO NLC (0.5 ± 0.50) in a treated group of animals. Hence, it can be concluded that MZ, through an optimized NLC of SO, can treat candidiasis effectively by inhibiting the growth of C. albicans .

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“…The effects of the AgNMS complex in SSCC treatment in a transdermal device was also expected in this study, since topic treatment of the SSCC with niosomal system, made up of alpha,omega-hexadecyl-bis-(1-aza-18-crown-6), for delivery of 5-fluorouracil [50], 5-fluorouracil, imiquimod, diclofenac, ingenolmebutate, retinoids, resiquimod, piroxicam, dobesilate, and betulinic acid [51] were early described. Also, drug-loaded nanostructured lipid carrier gel of quercetin and resveratrol [52], dermal targeted combinatorial lipid nanocolloidal based formulation of 5-fluorouracil and resveratrol [53], and silver nanoparticles with sericin and chitosan [54] have been noticed with great interest in the medical literature. It is worth mentioning that the low cost and complexity involved in the AgNMS@BCM preparation may confer an advantage for this device among others in the SSCC treatment.…”

Section: Discussionmentioning

confidence: 99%

“…It is also important to mention that a growing interest in the topic treatment of SSCC has been observed in the last decade. The aim of this kind of treatment is to avoid mutilations imposed by surgery and toxic effects of systemic treatments [50][51][52][53][54]. The most common topic agents used in treatment of SSCC patients is 5-fluorouracil (5-FU) [55][56][57] and imiquimod [57].…”

Section: Introductionmentioning

confidence: 99%

Silver Nimesulide Complex in Bacterial Cellulose Membranes as an Innovative Therapeutic Method for Topical Treatment of Skin Squamous Cell Carcinoma

et al. 2022

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Oxidative stress and inflammation act on skin squamous cell carcinoma (SSCC) development and progression. Curative therapy for SSCC patients is mainly based on surgical resection, which can cause various sequelae. Silver ions have in vitro activities over tumor cells, while nimesulide has antioxidant and anti-inflammatory activities. This study aimed to evaluate the effects of a silver(I) complex with nimesulide (AgNMS) incorporated in a sustained release device based on bacterial cellulose membrane, named AgNMS@BCM, on topic SSCC treatment. The antiproliferative effect of AgNMS complex was evaluated in the SCC4, SCC15 and FaDu SCC lines. AgNMS complex activity on exposure of phosphatidylserine (PS) residues and multicaspase activation were evaluated on FaDu cells by flow cytometry. The AgNMS@BCM effects were evaluated in a SSCC model induced by 7,12-dimethylbenzanthracene/12-o-tetradecanoyl-phorbol-13-acetate (DMBA/TPA) in mice. Toxicity and tumor size were evaluated throughout the study. AgNMS complex showed antiproliferative activity in SCC15 and FaDu lines in low to moderate concentrations (67.3 µM and 107.3 µM, respectively), and induced multicaspase activation on FaDu cells. The AgNMS@BCM did not induce toxicity and reduced tumor size up to 100%. Thus, the application of AgNMS@BCM was effective and safe in SSCC treatment in mice, and can be seen as a potential and safe agent for topic treatment of SSCC in humans.

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Topical nanostructured lipid carrier gel of quercetin and resveratrol: Formulation, optimization, in vitro and ex vivo study for the treatment of skin cancer

Cited by 134 publications

References 58 publications

UHPLC-MS Chemical Fingerprinting and Antioxidant, Antiproliferative, and Enzyme Inhibition Potential of Gaultheria pumila Berries

UHPLC-MS Chemical Fingerprinting and Antioxidant, Antiproliferative, and Enzyme Inhibition Potential of Gaultheria pumila Berries

Development, optimization, and evaluation of a nanostructured lipid carrier of sesame oil loaded with miconazole for the treatment of oral candidiasis

Silver Nimesulide Complex in Bacterial Cellulose Membranes as an Innovative Therapeutic Method for Topical Treatment of Skin Squamous Cell Carcinoma

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