Improved oral bioavailability of capsaicin via liposomal nanoformulation: preparation, in vitro drug release and pharmacokinetics in rats

Abstract

This study innovatively prepared an effective capsaicin-loaded liposome, a nanoformulation with fewer irritants, for oral administration. The in vitro and in vivo properties of the liposomal encapsulation were investigated and the potential possibility of oral administration evaluated. The liposomal agent composed of phospholipid, cholesterol, sodium cholate and isopropyl myristate was prepared using film-dispersion method. A level A in vitro-in vivo correlation (IVIVC) was established for the first time, which demonstrated an excellent IVIVC of both formulated and free capsaicin in oral administration. Physicochemical characterizations including mean particle size, zeta (ζ) potential and average encapsulation efficiency of capsaicin-loaded liposome were found to be 52.2 ± 1.3 nm, -41.5 ± 2.71 mv and 81.9 ± 2.43 %, respectively. In vivo, liposomal encapsulation allowed a 3.34-fold increase in relative bioavailability compared to free capsaicin. The gastric mucosa irritation studies indicated that the liposomal system was a safe carrier for oral administration. These results support the fact that capsaicin, an effective drug for the treatment of neuropathic pain, could be encapsulated in liposome for improved oral bioavailability. The excellent IVIVC of capsaicin-loaded liposome could also be a promising tool in liposomal formulation development with an added advantage of reduced animal testing.

Fucose decorated solid-lipid nanocarriers mediate efficient delivery of methotrexate in breast cancer therapeutics

“…Structurally, phospholipid resembles the lipid membrane of living cells. The amphiphilic characteristic allows them to form organized structures, such as carriers or membranes of lipid bilayer, when injected into an aqueous environment (stirring) [12]. Phospholipid based carries reveled features include higher encapsulation efficiency (EE) and oral bioavailability, non-toxicity, and better biocompatibility and stability compared with traditional liposomes [13].…”

Dietary Phytochemicals as Cancer Preventive Agents: Efficacy and Mechanisms

“…The particles also resulted in 27-fold higher AUC than that of curcumin powder in healthy human volunteers, theracurmin (30 mg) when administered orally [143]. Capsaicin is also able to be encapsulated in liposome, which shows improved oral bioavailability [127].…”

“…Capsaicin is also known to have low bioavailability, which is associated with poor water solubility and a short half-life [126,127]. On the other hand, it has been reported that over 90% of capsaicin can be absorbed rapidly and reach the peak concentration at 1 h after administration in rats [128].…”

“…Those include nanoparticles, liposomes, micelles, and phospholipid complex [127,140,141]. Nanocurcumin indeed increases bioavailability of curcumin in animals as well as in humans.…”

Preparation and In Vitro–In Vivo Evaluation of Sustained-Release Matrix Pellets of Capsaicin to Enhance the Oral Bioavailability

“…Therefore, developing a novel oral preparation of capsaicin has become imperative. In light of this, recently, a number of formulation strategies including nanoemulsion (20), liposome (21), and micelle (22) have been employed to solubilize and to enhance the oral bioavailability while without the effect of sustained release. In spite of these developments, exploiting the full clinical application of capsaicin is far from being optimized.…”