Aceclofenac-Soluplus&reg Nanocomposites for Increased Bioavailability

Abstract

Aceclofenac is a new generational Non-Steroidal Anti-Inflammatory Drug (NSAID), and is considered a better alternative to the popular painkiller diclofenac, as it overcomes some of the adverse gastrointestinal and cardiac side effects associated with the latter. However, the bioavailability of the drug remains limited due to low aqueous solubility (0.058 µg/mL) and poor dissolution characteristics. Hence, improving its dissolution characteristics is of prime significance in order to establish its optimal therapeutic efficacy. In an effort to tackle this issue, we report the use of novel Soluplus ®-based nanocomposites, prepared from emulsion templates, as effective drug loading agent for aceclofenac. Nanoemulsion templates were prepared by high-shear homogenization using a probe sonicator. The emulsions were subsequently lyophilized to obtain free flowing powders. The amorphization of the drug with increasing polymer content was clearly observed from powder X-ray diffractogram, while the drug-polymer interaction was explored by FTIR spectroscopy. The phase purity and homogeneity of the formulation was characterized using Differential Scanning Calorimetry. The dissolution profiles of the formulations were established by an USP paddle apparatus. Phase solubility study was conducted to evaluate the effect of polymer concentration on aqueous solubility of aceclofenac. The values of Gibbs-free energy (ΔG˚tr) associated with the aqueous solubility of aceclofenac in the presence of Soluplus was used to optimize the polymer content. The in vitro dissolution rates of aceclofenac from the nanoparticles were significantly higher compared to the pure drug. Thus, Soluplus nanoparticles provide promising formulations for the improvement of the dissolution profiles and thus, the bioavailability, of aceclofenac.

Zein nanoparticle‐embedded electrospun PVA nanofibers as wound dressing for topical delivery of anti‐inflammatory diclofenac

“…The physical state of an active pharmaceutical ingredient can significantly influence its bioavailability and stability. The bioavailability of drugs may remain limited due to their low aqueous solubility . The drug is dispersed, either in a crystalline or amorphous form in the polymeric matrix during formulation of the NPs.…”

A top-down technique to improve the solubility and bioavailability of aceclofenac: in vitro and in vivo studies

“…29 There is another literature on ACF-Soluplus ® nanocomposites by high-shear homogenization using a probe sonicator. 31 Nevertheless, most of these methods use many excipients that may be an economic burden. Also, researchers have used probe-sonication as the tool for size control.…”

Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen

“…Gelucire 44/14, thus, has interesting properties due to its unique combination of surfactants (mono and diesters of polyethylene glycol), cosurfactants (monoglycerides), and oily phase (diglycerides and triglycerides). The incorporation of gelucires in drug formulations has been reported to increase the dissolution rate of poorly soluble drugs such as aceclofenac [17], piroxicam [18] and glibenclamide [19] leading to an improved drug bioavailability…”

“…Gelucire 50/13 (the number relates to its melting point and hydrophilic-lipophilic balance value) is semi-solid lipid based solubilizer, manufactured by Gattefose, France. Chemically, it is a mixture of several glycerides (mainly C16/18) and mono and diesters of PEG 1500 (stearoyl polygyceride) [18,19]. These polymers form water-soluble complexes with many drug molecules, depending on the chemical structure of the Active Pharma Ingradients (APIs) [20].…”