Glucocorticoid entrapment into lipid carriers — characterisation by parelectric spectroscopy and influence on dermal uptake

Abstract

Topical glucocorticoids such as betamethasone 17-valerate (BMV) and prednicarbate (PC) are an important therapeutic option in atopic eczema. To reduce the risk of dermal atrophy, we aimed at BMV incorporation into solid lipid nanoparticles (SLN) for epidermal targeting using various lipids and emulsifiers corresponding to previous work on PC. Cutaneous absorption into excised human skin was compared to the one with a cream. While Compritol-based particles increased BMV uptake about fourfold we failed, however, to obtain epidermal targeting. To obtain insight into the location of active substance relative to the carrier, we used the recently optimised method of parelectric spectroscopy (PS). In fact, we were able to study electric dipole movements in the broad field of a frequency span from 0.1 to 100 MHz demonstrating that glucocorticoids are attached to the particle surface but are not incorporated into the lipid matrix. With BMV, the loading capacity of the particle surface lies clearly below the usual concentration of 0.1% which is not the case with PC. An adequate association of drug and carrier is essential for epidermal targeting. Parelectric spectroscopy provides insight into the interaction between drug and lipidic carrier.

Design and development of solid lipid nanoparticles for topical delivery of an anti-fungal agent

“…Especially, SLN can favor drug penetration into the skins (Jenning et al, 2000;, maintain a sustained release to avoid systemic absorption (Zur Muhlen et al, 1998), act as a UV sunscreen system (Wissing & Muller, 2002a), and reduce irritation (Maia et al, 2000;Sivaramakrishnan et al, 2004). It was used for topical delivery of several drugs including clotrimazole, flurbiprofen, prednicarbate, and betamethasone 17-valerate, and SLN also was reported to have skin targeting potential (Maia et al, 2000;Sivaramakrishnan et al, 2004;Jain et al, 2005;Song & Liu, 2005). SLN was found to have skin targeting which can result in a high accumulation of podophyllotoxin in the skin (Chen et al, 2006).…”

Structure and dynamics of drug-carrier systems as studied by parelectric spectroscopy☆

“…(6). This model as described in detail [1] needs a maximum activation energy for zero drug concentration and for its maximum possible value; in between these limiting cases, the adjacent particles find places in the wholes between the guest molecules thus needing less activation energy when forced to jump.…”

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

“…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).…”