Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

Altamimi, Mohammad A.; Hussain, Afzal; Alshehri, Sultan; Imam, Syed Sarim; Alnemer, Usamah Abdulrahman

doi:10.3390/pharmaceutics13081218

Cited by 31 publications

(31 citation statements)

References 49 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…KTZ-CNM13 elicited higher permeation profile as compared to KTZ-ANM13 which may primarily be attributed to the imposed cationic nature of nanoscale globules for enhanced permeation through various mechanistic phenomenon involved and working together. 18 KTZ-CNM13 exhibited approximately 4 times greater permeation than KTZ-SUP. Moreover, higher permeation of KTZ-CNM13 is attributed to PG and LAB-mediated reversible perturbation and changes in the lipid-protein bilayer structure in skin layers.…”

Section: Resultsmentioning

confidence: 87%

“…However, the solubility study was conducted in various excipients. 18 KTZ belongs to a biopharmaceutics classification system class II with very slight solubility in acetate buffer (0.3 mg/mL). Therefore, it was required to analyze the solubility of KTZ in various excipients, viz., oil, surfactant, and cosurfactant, to identify the best excipients for formulating the cationic nanoemulsion.…”

Section: Methodsmentioning

confidence: 99%

“…In this study, OLA was anticipated to be adhered as a surface charge inducer which subsequently may result in a positive charge (ZP) for electrostatic repulsion amid nanoglobules of bulk formulation. 18 On the other hand, the undiluted samples were used to measure real-time ZP values at room temperature (Zetasizer Delsa Nano C, United States of America). The study was replicated for mean and standard values ( n = 3).…”

Section: Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Ketoconazole-Loaded Cationic Nanoemulsion: In Vitro–Ex Vivo–In Vivo Evaluations to Control Cutaneous Fungal Infections

et al. 2022

Self Cite

View full text Add to dashboard Cite

An attempt has been made to optimize ketoconazole (KTZ)-loaded cationic nanoemulsion for topical delivery followed by in vitro , ex vivo , and in vivo evaluations. Central composite design suggested a total of 13 outcomes at 3 factors and 2 levels against 6 responses. Formulations were characterized for globular size, polydispersity index, pH, ζ potential, % entrapment efficiency (% EE), and drug content. Moreover, the optimized KTZ-CNM13 was compared against drug suspension (KTZ-SUS), commercial cream, and anionic nanoemulsion for in vitro drug release, ex vivo permeation, in vitro hemolysis, antifungal assay, in vivo dermal irritancy, and long-term stability. KTZ-CNM13 was found to have a low size (239 nm), an optimal ζ potential (+22.7 mV), a high % EE (89.1%), a spherical shape, a high drug content (98.9%), and a high numerical desirability value (1.0). In vitro drug release behavior of KTZ from KTZ-CNM13 was 7.54- and 1.71-folds higher than those of KTZ-ANM13 and KTZ-SUS, respectively, at 24 h. The permeation rate values were ordered as KTZ-CNM13 > KTZ-ANM13 > KTZ-MKT > KTZ-SUP due to various studied factors. High values of zone of inhibition for KTZ-CNM13 were observed against Candida albicans , Candida glabrata , Candida tropicalis, and Candida krusei as compared to KTZ-SUS. In vitro hemolysis and in vivo irritation studied confirmed the safety concern of the nanoemulsion at the explored composition. Long-term stability result revealed a stable product at the explored temperature for a year. Conclusively, cationic nanoemulsion is a promising approach to deliver KTZ for high permeation and therapeutic efficacy.

show abstract

Section: Resultsmentioning

confidence: 87%

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

See 1 more Smart Citation

Ketoconazole-Loaded Cationic Nanoemulsion: In Vitro–Ex Vivo–In Vivo Evaluations to Control Cutaneous Fungal Infections

et al. 2022

Self Cite

View full text Add to dashboard Cite

show abstract

“…The quantitative assessment of LUT was performed using a validated high performance liquid chromatography (HPLC) technique [45]. In this, the packing material of the analytical column (150 mm × 4.5 mm) worked as stationary phase with particle size of 5 µm operating at 30 ± 1 • C. The sample was injected at low volume (20 µL) for 8 min (run time) at flow rate of 1 mL/min.…”

Section: Methodsmentioning

confidence: 99%

“…The drug analysis was conducted on an isocratic mode using a UV detector (350 nm as set wavelength). A working calibration curve was constructed over concentration range of 20-100 µg/mL with high regression coefficient (r 2 > 0.99) [45].…”

Section: Methodsmentioning

confidence: 99%

Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations

et al. 2021

Self Cite

View full text Add to dashboard Cite

The study aimed to prepare and optimize luteolin (LUT)-loaded transdermal elastic liposomes (LEL1-LEL12), followed by in vitro and ex vivo evaluations of their ability to control breast cancer. Various surfactants (Span 60, Span 80, and Brij 35), and phosphatidyl choline (PC) as a lipid, were used to tailor various formulation as dictated by “Design Expert® software (DOE). These were characterized for size, polydispersity index (PDI), and zeta potential. The optimized formulation (OLEL1) was selected for comparative investigations (in vitro and ex vivo) against lipo (conventional liposomes) and drug suspension (DS). Moreover, the in vitro anticancer activity of OLEL1 was compared against a control using MCF-7 cell lines. Preliminary selection of the suitable PC: surfactant ratio for formulations F1–F9 showed relative advantages of Span 80. DOE suggested two block factorial designs with four center points to identify the design space and significant factors. OLEL1 was the most robust with high functional desirability (0.95), minimum size (202 nm), relatively high drug release, increased drug entrapment (92%), and improved permeation rate (~3270 µg/cm2) as compared with liposomes (~1536 µg/cm2) over 24 h. OLEL1 exhibited a 6.2- to 2.9-fold increase in permeation rate as compared with DS (drug solution). The permeation flux values of OLEL1, and lipo were found to be 136.3, 64 and 24.3 µg/h/cm2, respectively. The drug disposition values were 670 µg, 473 µg and 148 µg, for OLEL1, lipo and DS, respectively. Thus, ex vivo parameters were significantly better for OLEL1 compared with lipo and DS which is attributed to the flexibility and deformability of the optimized formulation. Furthermore, OLEL1 was evaluated for anticancer activity and showed maximized inhibition as compared with DS. Thus, elastic liposomes may be a promising approach for improved transdermal delivery of luteolin, as well as enhancing its therapeutic efficacy in controlling breast cancer.

show abstract

Luteolin, a flavone ingredient: Anticancer mechanisms, combined medication strategy, pharmacokinetics, clinical trials, and pharmaceutical researches

Shi,

Chen,

Gong

et al. 2023

Phytotherapy Research

View full text Add to dashboard Cite

Current pharmaceutical research is energetically excavating the pharmacotherapeutic role of herb‐derived ingredients in multiple malignancies’ targeting. Luteolin is one of the major phytochemical components that exist in various traditional Chinese medicine or medical herbs. Mounting evidence reveals that this phytoconstituent endows prominent therapeutic actions on diverse malignancies, with the underlying mechanisms, combined medication strategy, and pharmacokinetics elusive. Additionally, the clinical trial and pharmaceutical investigation of luteolin remain to be systematically delineated. The present review aimed to comprehensively summarize the updated information with regard to the anticancer mechanism, combined medication strategies, pharmacokinetics, clinical trials, and pharmaceutical researches of luteolin. The survey corroborates that luteolin executes multiple anticancer effects mainly by dampening proliferation and invasion, spurring apoptosis, intercepting cell cycle, regulating autophagy and immune, inhibiting inflammatory response, inducing ferroptosis, and pyroptosis, as well as epigenetic modification, and so on. Luteolin can be applied in combination with numerous clinical anticarcinogens and natural ingredients to synergistically enhance the therapeutic efficacy of malignancies while reducing adverse reactions. For pharmacokinetics, luteolin has an unfavorable oral bioavailability, it mainly persists in plasma as glucuronides and sulfate‐conjugates after being metabolized, and is regarded as potent inhibitors of OATP1B1 and OATP2B1, which may be messed with the pharmacokinetic interactions of miscellaneous bioactive substances in vivo. Besides, pharmaceutical innovation of luteolin with leading‐edge drug delivery systems such as host–guest complexes, nanoparticles, liposomes, nanoemulsion, microspheres, and hydrogels are beneficial to the exploitation of luteolin‐based products. Moreover, some registered clinical trials on luteolin are being carried out, yet clinical research on anticancer effects should be continuously promoted.

show abstract

Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

Cited by 31 publications

References 49 publications

Ketoconazole-Loaded Cationic Nanoemulsion: In Vitro–Ex Vivo–In Vivo Evaluations to Control Cutaneous Fungal Infections

Ketoconazole-Loaded Cationic Nanoemulsion: In Vitro–Ex Vivo–In Vivo Evaluations to Control Cutaneous Fungal Infections

Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations

Luteolin, a flavone ingredient: Anticancer mechanisms, combined medication strategy, pharmacokinetics, clinical trials, and pharmaceutical researches

Contact Info

Product

Resources

About