Cyproterone Acetate Loading to Lipid Nanoparticles for Topical Acne Treatment: Particle Characterisation and Skin Uptake

Štecová, Jana; Mehnert, W.; Blaschke, Tobias; Kleuser, Burkhard; Sivaramakrishnan, R.; Zouboulis, Christos C.; Seltmann, Holger; Körting, Hans Christian; Kramer, K.D.; Schäfer‐Korting, Monika

doi:10.1007/s11095-006-9225-9

Cited by 118 publications

(50 citation statements)

References 44 publications

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“…29) No intact SLN and NLC penetrated into the skin, 31) therefore ATRA might be released from the nanoparticle the drug with or without permeation enhancers permeate through the skin. After application of the lipid nanoparticles onto the skin, film formation occurs, which subsequently leads to an occlusive effect.…”

Section: Skin Permeation and Skin Distribution Studymentioning

confidence: 99%

Terpene Composited Lipid Nanoparticles for Enhanced Dermal Delivery of All-<i>trans</i>-Retinoic Acids

Charoenputtakun

Pamornpathomkul

Opanasopit

et al. 2014

Biological & Pharmaceutical Bulletin

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In the present study, terpene composited lipid nanoparticles and lipid nanoparticles were developed and evaluated for dermal delivery of all-trans-retinoic acids (ATRA). Terpene composited lipid nanoparticles and lipid nanoparticles were investigated for size, size distribution, zeta potential, entrapment efficiency, photostability, and cytotoxicity. In vitro skin permeation of ATRA lipid formulations were also evaluated. To explore the ability of lipid nanocarriers to target the skin, the distribution of rhodamine B base in the skin was investigated using confocal laser scanning microscopy (CLSM). The results indicated that the physicochemical characteristics of terpene composited lipid nanoparticles influenced skin permeability. All lipid nanocarriers significantly protected ATRA from photodegradation and were non-toxic to normal human foreskin fibroblast cells in vitro. Solid lipid nanoparticles containing 10% limonene (10% L-SLN) had the highest ATRA skin permeability. Terpene composited SLN and nanostructured lipid carriers (NLC) showed higher epidermal permeation of rhodamine B across the skin based on CLSM image analysis. Our study suggests that terpene composited SLN and NLC can be potentially used as dermal drug delivery carriers for ATRA.Key words lipid nanoparticle; terpene; dermal delivery; all-trans-retinoic acid Transdermal drug delivery has been chosen as a feasible alternative route of drug delivery due to its various advantages over conventional oral and intravenous routes such as reduction of drug metabolism via first pass effect, minimization of pain, and possible controlled drug release.1,2) However, the effectiveness of transdermal drug delivery depends on the capability of drugs to penetrate across the skin in sufficient amounts to reach therapeutic levels.3) The stratum corneum is an important barrier of the skin for drug absorption. 4,5) To facilitate drug delivery through the skin, penetration enhancers, which ideally cause a temporary reversible reduction in the barrier function of the stratum corneum, are extensively used to increase percutaneous absorption. 6) Terpenes are a series of naturally occurring compounds consisting of isoprene (C 5 H 8 ) units. They have been used in transdermal research since 1960s as skin permeation enhancers. They are reported to be a very safe and are an effective class of penetration enhancers that has been classified by the Food and Drug Administration (FDA) as generally regarded as safe (GRAS).7) Limonene is a hydrocarbon lipophilic terpene obtained from the lemon peel of citrus lemon.8) Previous studies have demonstrated that permeability enhancement by limonene can occur through multiple possible mechanisms, which may have contributed to the enhanced permeability of ketoprofen.9) 1,8-Cineole, a terpene, has also been used to promote percutaneous absorption of several lipophilic drugs through hairless mouse skin 10,11) and was recently reported to have an enhancing effect on percutaneous Zidovudine (AZT) absorption across rat skin.12) The mechanism o...

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Section: Skin Permeation and Skin Distribution Studymentioning

confidence: 99%

Terpene Composited Lipid Nanoparticles for Enhanced Dermal Delivery of All-<i>trans</i>-Retinoic Acids

Charoenputtakun

Pamornpathomkul

Opanasopit

et al. 2014

Biological & Pharmaceutical Bulletin

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“…Penggunaan lain sistem pembawa NLC dapat diterapkan dalam kosmetik dan produk dermal (Pardeike, et al, 2009). Beberapa contoh bahan aktif obat yang digunakan dalam penerapan NLC antara lain: topical glucocorticoids (Sivaramakrishnan, et al, 2004), anti androgen (Stecova, et al, 2007), dan anti fungal (Souto, et al, 2004), anti inflamasi (Phatak & Chaudhari, 2013), dan sistem penghantaran obat pelepasan terkontrol dalam sistem NLC untuk meloxicam (Khurana, et al, 2013 (Khurana, 2013), celecoxib (Joshi, 2008), dan progesteron (Yuan, et al, 2007).…”

Section: Meloxicam Merupakan Golonganunclassified

Pengembangan Sistem Nanostructured Lipid Carriers (NLC) Meloxicam dengan Lipid Monostearin dan Miglyol 808 Menggunakan Metode Emulsifikasi

Annisa

Hendradi

Melani

2016

J. Trop. Pharm. Chem.

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“…Moreover, the drug dissolved or finely dispersed within the lipid matrix of the carrier or attached to the carrier surface should facilitate drug dissolution within epidermal lipids. Finally, a lipid film covering the skin surface may further enhance dermal absorption because of an additional occlusive effect (39). Penetration profiles depend on the chemical nature of drug molecules, size and structure of the nanoparticles (22).…”

Section: Determination Of Human Percutaneous Absorption Of It After Imentioning

confidence: 99%

Improved photostability, reduced skin permeation and irritation of isotretinoin by solid lipid nanoparticles / Povećana fotostabilnost, smanjena permeacija i iritacija izotretinoina iz kruto-tekućih nanočestica

Golmohammadzadeh¹,

Somaye²,

Reza³

2012

Acta Pharmaceutica

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Isotretinoin (IT) is used orally for the treatment of severe acne that has not responded to other measures. IT has also been tried in a number of other skin disorders and in some forms of neoplastic disease. It has obvious adverse side effects in oral administration. The most common is dryness of the mucous membranes, visual disturbances, skeletal hyperostosis, and musculoskeletal symptoms. Elevation of serum triglycerides, blood glucose and hepatic enzymes has also been reported (1, 2). However, topical preparations of IT are available, such as creams and gels that show systemic absorption. The topical utility of IT is strongly limited by several disadvantages, such as skin irritation, very low water solubility, and high instability in the presence of light, air and heat. The aim of this study was to develop new solid lipid nanoparticles of isotretinoin (IT-SLNs) and evaluate the ability of IT-SLNs to improve photostability, reduce skin permeation and irritating effects. IT-SLNs were prepared by the hot high pressure homogenization method. Size, zeta potential and morphological characteristics of the preparations were assessed by transmission electron microscopy (TEM) and thermotropic properties with differential scanning calorimetry (DSC). IT-SLNs had a small average diameter of 74.05 ± 8.91 nm and high encapsulation efficiency (EE) of 80.6 ± 1.2 %. The results showed that the entrapment of IT into SLNs reduced significantly its photodegradation. The in vitro permeation data showed that IT-SLNs can accumulate in the different layers of the skin and prevent systemic uptake of IT in mouse skin. IT-SLNs also significantly increased IT accumulation in the different layers of the stratum corneum of human skin. IT-SLN formulation was significantly less irritating compared to commercial IT-GEL, which shows its potential for improving skin tolerability and being a carrier for topical delivery of IT.

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Cyproterone Acetate Loading to Lipid Nanoparticles for Topical Acne Treatment: Particle Characterisation and Skin Uptake

Abstract: With particulate systems topical CPA treatment may be an additional therapeutic option for acne and other diseases of the pilosebaceous unit.

Cited by 118 publications

References 44 publications

Terpene Composited Lipid Nanoparticles for Enhanced Dermal Delivery of All-<i>trans</i>-Retinoic Acids

Terpene Composited Lipid Nanoparticles for Enhanced Dermal Delivery of All-<i>trans</i>-Retinoic Acids

Pengembangan Sistem Nanostructured Lipid Carriers (NLC) Meloxicam dengan Lipid Monostearin dan Miglyol 808 Menggunakan Metode Emulsifikasi

Improved photostability, reduced skin permeation and irritation of isotretinoin by solid lipid nanoparticles / Povećana fotostabilnost, smanjena permeacija i iritacija izotretinoina iz kruto-tekućih nanočestica

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