Boosting the In Vivo Transdermal Bioavailability of Asenapine Maleate Using Novel Lavender Oil-Based Lipid Nanocapsules for Management of Schizophrenia

Abstract

Lipid nanocapsules (LNCs) are promising for transdermal drug delivery due to their higher permeability-enhancing effects compared to polymeric nanoparticles. Lavender oil is an essential oil consisting of several terpenes (primarily linalool and linalyl acetate) known for their profound permeation-enhancing action. In the present work, we successfully encapsulated asenapine maleate (a second-generation antipsychotic that is highly metabolized by the liver, reducing its oral bioavailability) into biocompatible LNCs for transdermal application using a novel oily phase, i.e., lavender oil (LO-LNCs). A comparative study was conducted to determine the effects of different oily phases (i.e., Miglyol® 812, Labrafil® M1944CS, and Labrafac™ PG) on the LNCs. Surfactant types (Kolliphor® HS15, Kolliphor® EL and Tween80) and oil:surfactant ratios were studied. Blank and asenapine-loaded LNCs were optimized for particle size, polydispersity index, zeta potential, drug content and ex vivo skin permeation. Lavender oil and Labrafil® showed smaller vesicular sizes, while LO-LNCs increased the permeation of ASP across rat skin. In vivo pharmacokinetics revealed that LO-LNCs could increase the ASP Cmax via transdermal application by fourfold compared to oral suspension. They increased the bioavailability of ASP by up to 52% and provided sustained release for three days. The pharmacokinetic profile of the LO-LNCs was compared to ASP-loaded invasomes (discussed in a previous study) to emphasize LNCs’ transdermal delivery behavior.

Can Essential Oils/Botanical Agents Smart-Nanoformulations Be the Winning Cards against Psoriasis?

“…It is evident that polymeric nanoparticles, especially those having a particle size less than 100 nm and carrying a charge, are an excellent choice for the treatment of inflammatory skin disorders due to the selective accumulation in the inflamed skin [ 136 , 137 , 138 ]. On the other side, lipidic systems such as lipid nanoemulsions and nanocapsules tend to enhance the transdermal permeation of the encapsulated drugs due to their greater ability to diffuse through the different skin layers [ 139 , 140 ]. Therefore, polymeric nanocapsules containing natural oils would offer an excellent candidate for topical therapy.…”

Brain targeted lactoferrin coated lipid nanocapsules for the combined effects of apocynin and lavender essential oil in PTZ induced seizures

“…Increasing the proportion of LAV in LNC resulted in a decrease in PS with an increase in PDI but the difference was only statistically significant (p ≤ 0.05) when the proportion of LAV exceeded that of Labrafac (1:2; Labrafac: LAV ratio, F4). El-Tokhy et al, [65] previously reported smaller PS for LNC with Lavander essential oil oily core compared to Labrafac. This was attributed to Lavender oil low viscosity and low oil/water interfacial tension in addition to its polarity and hence ability to form nanoemulsions by the phase-inversion method [65].…”

“…El-Tokhy et al, [65] previously reported smaller PS for LNC with Lavander essential oil oily core compared to Labrafac. This was attributed to Lavender oil low viscosity and low oil/water interfacial tension in addition to its polarity and hence ability to form nanoemulsions by the phase-inversion method [65].…”

“…Colloidal properties of LNC were previously shown to be dependent on composition (Oil: SAA ratio) with particle size ranging from 25 to 100 nm [63][64][65]. Table 1 shows the PS, PDI and ZP of LNC.…”

Medicinal Anti-Inflammatory Patch Loaded with Lavender Essential Oil

“…Its analgesic effect is due to the content of compounds such as linalool and linalyl acetate, which have the ability to block the transmission of pain signals within the peripheral nervous system [ 27 , 28 , 29 ]. Moreover, previous studies have demonstrated the potential of lavender essential oil as an effective carrier for drug delivery, enhancing the permeation and therapeutic efficacy of various pharmaceuticals, such as asenapine maleate [ 30 ], penciclovir [ 31 ], lidocaine, caffeine [ 32 ], and p-aminobenzoic acid [ 18 ]. The use of essential oils such as clove, cinnamon, cyperus, chuanxiong, angelica, and turpentine [ 13 , 17 , 33 ] in increasing ibuprofen’s bioavailability is also known.…”