Nanostructured lipid carriers of pioglitazone for transdermal application: from experimental design to bioactivity detail

Abstract

Pioglitazone (PZ) an anti-hyperglycemic agent is used in the treatment of type 2 diabetes. The aim of this study was to design PZ-loaded nanostructured lipid carriers (NLC) to investigate the bioavailability improvement by transdermal delivery. PZ NLCs were prepared using highpressure homogenization followed by ultrasonication. The NLCs were evaluated for particle size analysis, drug loading, ex vivo skin transport studies and in vivo bioactivity study. The prepared NLCs had a mean size of 166.05 nm and drug loading of 10.41% with flux value of 47.36 mg/cm 2 /h. The entrapment of PZ is 470% in the NLCs with enhancement ratio of 3.2 times. The in vivo pharmacokinetic study showed 2.17 times enhancement in bioavailability study and pharmacodynamics study showed that PZ NLC-based transdermal therapeutic system (PNLG-TTS) lowers blood sugar level in a sustained pattern for a prolonged period of time as compared to Piosys tablet (marketed). The shelf life of the optimized formulation was found to be 1.83 years. These results clearly provide a lead that above NLCs-based TTS is potential controlled release formulation for PZ and could be a promising drug delivery system for the treatment of diabetes.

Transcriptional transactivator peptide modified lidocaine-loaded nanoparticulate drug delivery system for topical anesthetic therapy

“…When compared with LID solution, TAT-NLCs-LID and NLCs-LID improved the permeation of LID 3.8-fold and 2-fold in 48 h, respectively. The results illustrated that NLCs formulas have better skin permeation capacity, which may be due to their similar property to skin lipids, the high specific surface area for drug absorption because of their smaller size in nanometric range, the existence of a solid matrix and the biocompatibility which make them suitable for long-term skin administration (Alam et al, 2016;Vitorino et al, 2014). When TAT was modified onto NLCs-LID, its penetration rate and flux were significantly higher (p50.05) than non-modified NLCs-LID at all time points studied.…”

“…Compared to injection pathway, transdermal drug delivery (TDD) of LA agents has the following advantages: improved patient compliance; fewer side effects; continuous drug delivery; avoiding the hepatic first pass effect (Trotta et al, 2002;Wang et al, 2013). However, the main challenge in TDD is to overcome the barrier of the stratum corneum (the outermost layer of the skin) for most of the incoming substances (Alam et al, 2016;Vitorino et al, 2014). Thus, there is a compelling need for rapid and effective local transdermal anesthetics.…”

“…NLCs are colloidal carriers characterized by a solid lipid core consisting of a mixture of solid and liquid lipids (Doktorovova & Souto, 2009;Müller et al, 2011). Because of their special structure, NLCs have higher loading capacity and lower drug leaching on storage compared to other lipid nanocarriers; moreover, their chemical similarity to skin lipids, stemming from the common hydrophobic character, the high specific surface area for drug absorption because of their smaller size in nanometric range, the existence of a solid matrix and the biocompatibility make them suitable for long-term skin administration (Alam et al, 2016;Vitorino et al, 2014).…”

Local anesthetic lidocaine delivery system: chitosan and hyaluronic acid-modified layer-by-layer lipid nanoparticles

“…Data show that the permeation of LA in LA/NLCs was much more sufficient than LA solutions (p50.05). The results illustrated that NLCs formulas have better skin permeation capacity, which may be due to their similar property to skin lipids, the high specific surface area for drug absorption because of their smaller size, the existence of a solid matrix and the biocompatibility make them suitable for skin administration (Vitorino et al, 2013;Alam et al, 2014). The permeation of LBL-LA/NLCs was more sufficient than HA-LA/NLCs (p50.05); and permeation of HA-LA/NLCs was more sufficient than LA/NLCs (p50.05).…”

Transdermal delivery of antidiabetic drugs: formulation and delivery strategies

“…Further authors claimed that the prepared formulation showed 2.17-times enhancement in bioavailability of Pz in comparison with control formulation. The shelf-life of 1.83 years was assigned to Pz in developed lipid carrier systems [57].…”