Preparation and Characterization of Nanostructured Lipid Carriers for Improved Topical Drug Delivery: Evaluation in Cutaneous Leishmaniasis and Vaginal Candidiasis Animal Models

Riaz, Arshad; Hendricks, Sarah A.; Elbrink, Kimberley; Caljon, Guy; Maes, Louis; Ahmed, Naveed; Kiekens, Filip; Khan, Gul Majid

doi:10.1208/s12249-020-01717-w

Cited by 21 publications

(40 citation statements)

References 68 publications

(15 reference statements)

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“…The variation in pH value may lead to skin irritation. The prepared LT-NVoptG had a pH value of 6.6 ± 0.44, which is within the limit of skin formulation and does not produce any toxicity [47]. The viscosity is also one of the important parameters for the semisolid formulation.…”

Section: Characterization Of Gelmentioning

confidence: 93%

Formulation, Optimization and Evaluation of Luteolin-Loaded Topical Nanoparticulate Delivery System for the Skin Cancer

et al. 2021

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In the present study, luteolin (LT)-loaded nanosized vesicles (LT-NVs) were prepared by a solvent evaporation–hydration method using phospholipid and edge activator. The formulation was optimized using three factors at a three-level Box–Behnken design. The formulated LT-NVs were prepared using the three independent variables phospholipid (A), edge activator (B) and sonication time (C). The effect of used variables was assessed on the vesicle size (Y1) and encapsulation efficiency (Y2). The selection of optimum composition (LT-NVopt) was based on the point prediction method of the software. The prepared LT-NVopt showed the particle size of 189.92 ± 3.25 nm with an encapsulation efficiency of 92.43 ± 4.12% with PDI and zeta potential value of 0.32 and −21 mV, respectively. The formulation LT-NVopt was further converted into Carbopol 934 gel (1% w/v) to enhance skin retention. LT-NVoptG was further characterized for viscosity, spreadability, drug content, drug release, drug permeation and antioxidant, antimicrobial and cytotoxicity assessment. The evaluation result revealed optimum pH, viscosity, spreadability and good drug content. There was enhanced LT release (60.81 ± 2.87%), as well as LT permeation (128.21 ± 3.56 µg/cm2/h), which was found in comparison to the pure LT. The antioxidant and antimicrobial study results revealed significantly (p ˂ 0.05) better antioxidant potential and antimicrobial activity against the tested organisms. Finally, the samples were evaluated for cytotoxicity assessment using skin cancer cell line and results revealed a significant difference in the viability % at the tested concentration. LT-NVoptG showed a significantly lower IC50 value than the pure LT. From the study, it can be concluded that the prepared LT-NVoptG was found to be an alternative to the synthetic drug as well as conventional delivery systems.

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Section: Characterization Of Gelmentioning

confidence: 93%

Formulation, Optimization and Evaluation of Luteolin-Loaded Topical Nanoparticulate Delivery System for the Skin Cancer

et al. 2021

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“…The pH of BF-NLCopt gel was determined by pH meter at room temperature and the value was found to be 6.5 ± 0.2. The pH was found to be within the limit of topical gel and does not produce any toxicity [ 7 ]. The viscosity of BF-NLCopt gel was evaluated by Brookfield viscometer and the result was found to be 519 ± 1.43 CPs.…”

Section: Resultsmentioning

confidence: 99%

“…These delivery systems improve the therapeutic efficacy by a different mechanism including enhancing permeation through subcutaneous, enhanced solubility, sustained drug release, and targeting potential to macrophage, and deeper skin layer [ 5 , 6 ]. Nano lipid carrier (NLC) is a second-generation lipid formulation prepared with a blend of solid lipid and liquid lipid [ 7 ]. They are prepared with physiological solid and liquid lipid, which is completely biodegradable.…”

Section: Introductionmentioning

confidence: 99%

“…The gel system should be washable, non-staining, stable at room temperature, and should not affect the biological nature of the drug [ 15 ]. There are numerous NLCs-based topical systems that have been reported to enhance the therapeutic efficacy of poorly soluble drugs like valdecoxib [ 11 ], luliconazole [ 16 , 17 ], oxiconazole [ 18 ], amphotericin B [ 7 ], itraconazole [ 19 ].…”

Section: Introductionmentioning

confidence: 99%

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Formulation and Optimization of Butenafine-Loaded Topical Nano Lipid Carrier-Based Gel: Characterization, Irritation Study, and Anti-Fungal Activity

et al. 2021

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The present study aims to prepare and optimize butenafine hydrochloride NLCs formulation using solid and liquid lipid. The optimized selected BF-NLCopt was further converted into Carbopol-based gel for topical application for the treatment of fungal infection. Box Behnken design was employed to optimize the nanostructure lipids carriers (NLCs) using the lipid content (A), Tween 80 (B), and homogenization cycle (C) as formulation factors at three levels. Their effects were observed on the particle size (Y1) and entrapment efficiency (Y2). The selected formulation was converted into gel and further assessed for gel characterization, drug release, anti-fungal study, irritation study, and stability study. The solid lipid (Compritol 888 ATO), liquid lipid (Labrasol), and surfactant (tween 80) were selected based on maximum solubility. The optimization result showed a particle size of 111 nm with high entrapment efficiency of 86.35% for BF-NLCopt. The optimized BF-NLCopt converted to gel (1% w/v, Carbopol 934) and showed ideal gel evaluation results (drug content 99.45 ± 2.11, pH 6.5 ± 0.2, viscosity 519 ± 1.43 CPs). The drug release study result depicted a prolonged drug release (65.09 ± 4.37%) with high drug permeation 641.37 ± 46.59 µg (32.07 ± 2.32%) than BF conventional gel. The low value of irritation score (0.17) exhibited negligible irritation on the skin after application. The anti-fungal result showed greater efficacy than the BF gel at both time points. The overall conclusion of the results revealed NLCs-based gel of BF as an ideal delivery system to treat the fungal infection.

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“…The pH of BT-NPopG was found to be 6.6 ± 0.3, which is ideal for the topical formulation and does not produce any irritation (Riaz et al., 2020 ). The viscosity was also assessed to check the flow property of the prepared gel and the value was found to be 35,276 ± 14 cps.…”

Section: Resultsmentioning

confidence: 99%

Formulation and evaluation of butenafine loaded PLGA-nanoparticulate laden chitosan nano gel

Alshehri

Imam

2021

Drug Delivery

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Preparation and Characterization of Nanostructured Lipid Carriers for Improved Topical Drug Delivery: Evaluation in Cutaneous Leishmaniasis and Vaginal Candidiasis Animal Models

Cited by 21 publications

References 68 publications

Formulation, Optimization and Evaluation of Luteolin-Loaded Topical Nanoparticulate Delivery System for the Skin Cancer

Formulation, Optimization and Evaluation of Luteolin-Loaded Topical Nanoparticulate Delivery System for the Skin Cancer

Formulation and Optimization of Butenafine-Loaded Topical Nano Lipid Carrier-Based Gel: Characterization, Irritation Study, and Anti-Fungal Activity

Formulation and evaluation of butenafine loaded PLGA-nanoparticulate laden chitosan nano gel

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