Preparation, characterization and bioavailability by oral administration of O/W curcumin nanoemulsions stabilized with lysophosphatidylcholine

Abstract

Curcumin is the main and most abundant bioactive component in Curcuma longa L. with documented properties in the prevention and treatment of chronic degenerative and infectious diseases. However, curcumin has low solubility in aqueous media, hence low bioavailability when administered orally. The use of nanoemulsions as carriers can provide a partial solution to bioavailability restrictions. In our study, O/W nanoemulsions of curcumin were prepared using lysophosphatidylcholine, a phospholipid with proven emulsification capacity; nevertheless, such qualities have not been previously reported in the preparation of nanoemulsions. Lysophosphatidylcholine was obtained by enzymatic removal of one fatty acid residue from phosphatidylcholine. The objective of our work was to formulate stable curcumin nanoemulsions and evaluate their bioavailability in BALB/c mice plasma after oral administration. Formulated nanoemulsions had a droplet size mean of 154.32 ± 3.10 nm, a polydispersity index of 0.34 ± 0.07 and zeta potential of -10.43 ± 1.10 mV; stability was monitored for 12 weeks. Lastly, in vivo pharmacokinetic parameters, using BALB/c mice, were obtained; namely, C of 610 ± 65.0 μg mL and T of 2 h. Pharmacokinetic data revealed a higher bioavailability of emulsified as opposed to free curcumin. Research regarding other potential emulsifiers that may provide better health benefits and carry nano-encapsulated bioactive compounds more effectively, is necessary. This study provides important data on the preparation and design of nanoencapsulated Curcumin using lysophosphatidylcholine as an emulsifier.

Development of Theranostic Perfluorocarbon Nanoemulsions as a Model Non-Opioid Pain Nanomedicine Using a Quality by Design (QbD) Approach

“…This makes nanoemulsions an attractive candidate for study using QbD approaches that include mixture process variable design of experiments. Nanoemulsions are also promising carriers for anti-inflammatory drugs and/or natural products (9)(10)(11) and potential future pain nanomedicines. Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed to treat pain, as these drugs are non-addictive alternatives to opioids.…”

Current approaches in lipid-based nanocarriers for oral drug delivery

“…The different preparation methods to obtain nanoemulsions can be classified into high-energy or low-energy approaches. High-energy methods, such as ultrasonic homogenisation or microfluidisation, usually entail high formulation temperatures, what may limit their use of thermo labile molecules like peptides [73,74,77,[88][89][90][91][92][93][94]. Low-energy methods, including solvent displacement technique and phase inversion, are performed in milder conditions [74].…”

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

“…Nanoemulsions, another representative lipid nanocarrier, have also demonstrated a great potential in promoting oral absorption of poorly water-soluble drugs. Yin et al developed biocompatible nanoemulsions using hemp oil and less surfactants for the oral delivery of baicalein [ 93 ], and Chavez-Zamudio et al prepared lysophosphatidylcholine-stabilized nanoemulsions for the oral delivery of curcumin [ 176 ]. The constructed nanoemulsion systems unexceptionally enhanced the oral bioavailability of payloads in comparison with their coarse dispersions.…”