Table 4.
Delivery of alkaloids derived from traditional Chinese medicine by transdermal drug delivery systems.
| Carrier types | Alkaloids | Carrier composition | Preparation | Method of model | Method of dosing | Effects | References |
|---|---|---|---|---|---|---|---|
| Ethosomes | Ligustrazine | Phospholipid, cholesterol, ethanol (1:0.4:45) or egg phosphatidylcholine, 30% ethanol (2.5:30) | Ethanol injection-sonication | SD rats | Transdermally | The ethosome patches: AUC ↑ 1.09-fold, t1/2β ↑ 8.79-fold, Tmax ↑ 0.89-fold, Cmax ↓ 68.64%, CL ↓ 52.62%; whole blood viscosity ↓, plasma viscosity ↓, hematocrit ↓, RBC aggregation index ↓, RBC deformation index ↓, VF incidence ↓, times of ventricular premature beat ↓,SOD ↑, GSH-Px ↑, MDA ↓, the escape latency of amnesic rats ↓ | (Liu et al., 2011a,b; Shi et al., 2012b) |
| Tetrandrine | PC, ethanol, and propylene glycol | The pH gradient loading method | SD rats | Transdermally | The ethosomes: the drug flux of skin ↑ 1.1-fold, the drug deposition ↑ 0.7-fold; curing arthritis ↑ | (Fan et al., 2013) | |
| Penetration enhancers | Ligustrazine | Anethole or anisaldehyde or anisic acid or menthol and menthone | – | SD rats | Transdermally | The anisole compounds groups: percutaneous flux ↑, the apparent density ↑, Jss ↑, KP ↑ | (Zhang et al., 2015a; Wang et al., 2017) |
| Mesaconitine/Hypaconitine | M-OA | – | Male Wistar rats | Transdermally | The permeation ↑, desquamation of SC flake ↑, SC lipid fluidization ↑ | (Zhao et al., 2011) | |
| Solid lipid nanoparticles | Aconitine | Compritol® 888 ATO, Cremophor® EL), TranscotolP) | Microemulsion precursor method | SD rats | Transdermally | The SLNs: Cmax ↑ 2.56-fold, AUC0–10 h ↑ 1.26-fold, Tmax ↑ 3-fold than the ethanol tinctures; the AUC0–10 h and Cmax of the SLNs in scapular regin > abdomen > chest; the toxicity ↓, transdermal permeability ↑ | (Zhang et al., 2014b, 2015c) |
| Others | Ligustrazine | Oleic acid, Cremophor RH40, ethanol,1,8-cineole | The lamination technique | SD rats | Transdermally | The penetration ↑ | (Shi et al., 2012a) |
| Evodiamine/Rutaecarpine | Cremophor® EL, PEG400,Ethyl oleate,Water | – | SD rats | Transdermally | Evodiamine- and rutaecarpine-loaded microemulsions: the fluxes ↑ ; AUC0–10 h ↑ 2.06 and 3.23-fold | (Zhang et al., 2011) |
SD rats: male Sprague–Dawley rats; AUC: area under the concentration–time curve; t1/2β: elimination half-life; Cmax: maximum plasma concentration; Tmax: time to reach Cmax; CL: clearance; RBC: red blood cells; VF: ventricular fibrillation; SOD: superoxide dismutase; GSH-Px: glutathione peroxidase; MDA: Malondialdehyde; PC: Phosphatidylcholine; Jss: percutaneous flux; KP: permeability coefficients; M-OA: (E)-2-isopropyl-5-methylcyclohexyl octadec-9-enoate; SC: stratum corneum; SLNs: Solid lipid nanoparticles.