Dermatokinetic assessment of luliconazole-loaded nanostructured lipid carriers (NLCs) for topical delivery: QbD-driven design, optimization, and in vitro and ex vivo evaluations

Mahmood, Arisha; Rapalli, Vamshi Krishna; Gorantla, Srividya; Waghule, Tejashree; Singhvi, Gautam

doi:10.1007/s13346-021-00986-7

Cited by 45 publications

(28 citation statements)

References 54 publications

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“…s) and shear stress (τ). The data obtained were processed and analyzed using the instrument software RheoPlus, and the linear viscoelastic region (LVR) was determined using the amplitude sweep test by measuring G′ (storage modulus) and G″ (loss modulus) as a function of strain (%) ranging from 0.01 to 100% at a constant angular frequency of 1 and an angular velocity of 10 rad/sec (Chen et al, 2012;Jain et al, 2014;Romero De Avila et al, 2014;Mahmood et al, 2021).…”

Section: Rheological Behaviormentioning

confidence: 99%

“…The LVR provides information on the minimum strain required for the oscillation frequency sweep test that was carried out by measuring G′ and G″ as a function of angular frequency (rad/sec) at 0.1-100 rad/sec and a constant strain amplitude of 0.05 and 5% in the LVR (Mahmood et al, 2021). Following the abovementioned protocol, a test was carried out to monitor sample behavior at constant strain and changing frequency.…”

Section: Rheological Behaviormentioning

confidence: 99%

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Nanostructured Lipid Carrier–Mediated Transdermal Delivery of Aceclofenac Hydrogel Present an Effective Therapeutic Approach for Inflammatory Diseases

et al. 2021

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Aceclofenac (ACE), a cyclooxygenase-2 inhibitor, is the derivative of the diclofenac group that has been in use for the symptomatic treatment of systemic inflammatory autoimmune disease, rheumatoid arthritis (RA). Partial solubility, high lipophilic nature, and stability challenge its use in developing topical formulations. Hence, we developed and characterized nanostructured lipid carrier (NLC)–based ACE (ACE-NLC) hydrogel for an efficient transdermal delivery. NLC microemulsion was prepared using different lipids by various methods and was characterized with respect to particle size, zeta potential, surface morphology, and drug encapsulation efficiency. The optimized NLC formulation was incorporated into Carbopol® 940 gel, and this arrangement was characterized and compared with the existing marketed gel (Mkt-gel) formulation to assess in vitro drug release, rheology, texture profile, in vivo skin retention and permeation, and stability. Furthermore, prepared and characterized ACE-loaded NLC formulation was evaluated for skin integrity and fitted in a dermatokinetic model. The results of this study confirmed the spherical shape; smooth morphology and nanometric size attested by Zetasizer and scanning and transmission electron microcopy; and stability of the ACE-NLC formulation. The ACE-NLC-gel formulation showed good rheological and texture characteristics, and better skin distribution in the epidermis and dermis. Moreover, ACE-NLC permeated deeper in the skin layers and kept the skin integrity intact. Overall, NLC-based gel formulation of ACE might be a promising nanoscale lipid carrier for topical application when compared with the conventional Mkt-gel formulation.

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Section: Rheological Behaviormentioning

confidence: 99%

Section: Rheological Behaviormentioning

confidence: 99%

Nanostructured Lipid Carrier–Mediated Transdermal Delivery of Aceclofenac Hydrogel Present an Effective Therapeutic Approach for Inflammatory Diseases

et al. 2021

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“…NLCs have been also used as carriers for transdermal delivery due to the increase of solubility of water insoluble drug substances [4,[6][7][8][9][10]. A dermatokinetic assessment involved the administration of luliconazole-loaded NLCs with ultra-small particle size (< 100 nm) for antifungal activity [6].…”

Section: Introductionmentioning

confidence: 99%

In vivo evaluation of nanostructured lipid carrier systems (NLCs) in mice bearing prostate cancer tumours

Akanda

Getti

Douroumis

2021

Drug Deliv. and Transl. Res.

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Nanostructure lipid carriers (NLCs) were developed for the delivery of curmumin (CRN), a potent anticancer agent with low bioavailability, for the treatment of prostate cancer. NLCs prepared using high pressure homogenization (HPH) with around 150 nm particle size, − 40 V ζ-potential and excellent long-term stability. Cellular uptake of CRN-SLN showed nanoparticle localization in the cytoplasm around the nucleus. CRN-NLCs were assessed using flow cytometry and found to cause early and late apoptotic events at 100 μg/ml CRN concentrations. CRN-NLC nanoparticles were administrated to nude mice with LNCaP prostate cancer xenografts and demonstrated substantial tumour volume suppression (40%) with no weight loss compared to pure CRN (ethanolic solution). Overall, NLCs were proved a suitable carrier for passive drug delivery and cancer treatment. Graphical abstract

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Section: Introductionmentioning

confidence: 99%

“…NLCs have been also used as carriers for transdermal delivery due to the increase of solublity of water insoluble drug substances [4], [6]- [10]. A dermatokinetic assessment involved the administration of luliconazole loaded NLCs with ultra-small particle size (< 100nm) for antifungal activity [6]. Nanoparticles were loaded in a topical gel and clinical results showed 2-fold increase of Cmax and 3-fold for the AUC compared to a marketed cream.…”

Section: Introductionmentioning

confidence: 99%

In Vivo Evaluation of Nanostructured Lipid Carrier Systems (NLCs) in Mice Bearing Prostate Cancer Tumours

Akanda

Getti

Douroumis

2021

Preprint

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Nanostructure lipid carriers (NLCs) were developed for the delivery of curmumin (CRN), a potent anticancer agent with low bioavailability, for the treatment of prostate cancer. NLCs prepared using High Pressure Homogenization (HPH) with around 150 nm particle size, -40V ζ-potential and excellent long-term stability. Cellular uptake of CRN-SLN, showed nanoparticle localization in the cytoplasm around the nucleus. CRN-NLCs were assessed using flow cytometry and found to cause early and late apoptotic events at 100 μg/ml CRN concentrations. CRN-NLC nanoparticles were administrated to nude mice with LNCaP prostate cancer xenografts and demonstrated substantial tumour volume suppression (40%) with no weight loss compared to pure CRN (ethanolic solution). Overall, NLCs were proved a suitable carrier for passive drug delivery and cancer treatment.

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Dermatokinetic assessment of luliconazole-loaded nanostructured lipid carriers (NLCs) for topical delivery: QbD-driven design, optimization, and in vitro and ex vivo evaluations

Cited by 45 publications

References 54 publications

Nanostructured Lipid Carrier–Mediated Transdermal Delivery of Aceclofenac Hydrogel Present an Effective Therapeutic Approach for Inflammatory Diseases

Nanostructured Lipid Carrier–Mediated Transdermal Delivery of Aceclofenac Hydrogel Present an Effective Therapeutic Approach for Inflammatory Diseases

In vivo evaluation of nanostructured lipid carrier systems (NLCs) in mice bearing prostate cancer tumours

In Vivo Evaluation of Nanostructured Lipid Carrier Systems (NLCs) in Mice Bearing Prostate Cancer Tumours

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