No abstract

Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along with surfactant/co-surfactants, and the tablets were prepared by wet granulation using superdisintegrants and adsorbents. Infra-red (IR) spectral studies revealed no interaction between the drug and excipients, and all physical and chemical parameters were within acceptable limits. Stability studies for the formulation indicated no significant change over time. An in vitro release study indicated 100% drug release within 30 min, and in vivo plasma concentrations indicated that the area under the curve (AUC) of albendazole in rats administered SMEDDS chewable tablets was significantly higher than in those administered commercial tablets or powder (p-value < 0.05). The systemic bioavailability of albendazole achieved through the SMEDDS tablets was 1.3 times higher than that achieved by the administration of comparable quantities of albendazole commercial tablets. This was due to the higher dissolution of albendazole SMEDDS in the chewable tablets. We conclude that the SMEDDS chewable formulation can be used to improve the dissolution and systemic availability of poorly water-soluble drugs.

Techno-biofunctional characteristics of nanoemulsion and (nano)emulgel loaded with mangostin extracts were elucidated. Crude mangostins from mangosteen peels recovered by virgin coconut oil (VCO), mixed VCO and propylene glycol (PG), and pure PG were used. The extracts were loaded in the dispersed phase in the presence of mixed surfactants (Tween20/Span20) with a varying hydrophilic-lipophilic balance (HLB) from 10.2 to 15.1. Results showed that globular and uniformly distributed droplets of the nanoemulsion were observed. The small particle sizes (typically 18-62 nm) with the zeta potential of-39 to-54.5 mV were obtained when mixed emulsifiers with HLB values of 12.6 and 15.1 were employed. With HLB values of 12.6 and 15.1, nanoemulsions loaded with mangostin extracts prepared with mixed VCO-PG and pure PG-based extracts showed approximately a 2 to 3-fold lower droplet size diameter when compared with the VCO-based extract. For the stability test, all nanoemulsions were stable over three freeze-thaw cycles with some changes in pH, zeta potential, and droplet size. The DPPH • scavenging activity, H 2 O 2 scavenging activity, reducing power and antibacterial activities (E. coli and S. aureus) of the nanoemulsions were greater than their corresponding bulk extracts. Nanoemulgels produced by embedding the nanoemulsions in a hydrogel matrix was homogeneous and creamy yellow-white in appearance. The nanoemulgels had a higher mangostin release (87-92%) than their normal emulgels (74-78%). Therefore, this study presented the feasibility of nanoemulsions and nanoemulgels loaded with mangostin extracts as a promising delivery system for bioactive polyphenol in food supplements, pharmaceuticals and cosmetics.

Glochidion wallichianum (GW) is a good source of antioxidants, including gallic acid, promoting its development as a microemulsion. We constructed five pseudo-ternary phase diagrams comprising isopropyl myristate (IPM), water, and surfactant mixture (Smix)—i.e., Labrasol®:HCO-40® (1:1) with Transcutol® (1:1, 2:1, 3:1), and Tween80:Span80 (3:2) with Transcutol® or propylene glycol:ethanol (1:1). Additionally, blank and GW extract-loaded microemulsions were prepared at an IPM:Water:Smix ratio of 10:30:60 (high water content) and 30:10:60 (high oil content) from each Smix. The physical characteristics, skin permeation, and disposition were evaluated. The formulations with high water content and conductivities provided higher gallic acid permeation and disposition than those with high oil content. The Smix of Labrasol®:HCO-40® (1:1) and Transcutol® (1:1) promoted the highest gallic acid permeation (enhancement ratio 1.78 ± 0.12) and was suitable for transdermal delivery. However, the 1% hydroxypropyl methylcellulose control gel, the microemulsion with Smix of Labrasol®:HCO-40® (1:1) with Transcutol® (2:1), and Smix of Tween80:Span80 (3:2) with propylene glycol:ethanol (1:1) could provide higher skin accumulation of gallic acid than that with other formulations. The microstructures, ratio of surfactant:cosurfactant, and compositions of microemulsions were found to affect the skin permeation and disposition of gallic acid and require optimization to act as transdermal or topical delivery carriers.

Virgin coconut oil (VCO) and propylene glycol (PG) have received more attention as bio-based solvents for natural bioactive recovery in green extraction process.Here, maceration extraction and ultrasound-assisted extraction (UAE) of bioactive phenolics from mangosteen peel (MP) by VCO, PG and VCO-PG mixture were compared. The goal was to maximize the phenolic extraction and improve bioactivities. Based on a single-factor experiment for UAE with VCO, the optimal condition was sample to solvent ratio of 1:6.6 g/mL, amplitude of 55 lm, and extraction time of 7 min, which yielded total phenolic content of 365 mg GAE/100 g. Regarding the extraction methods and bio-based solvents, UAE with mixed VCO-PG was not only provided greater polyphenol yield in a shorter time, but it also enhanced the bioactivities (radical scavenging, antibacterial, and antidiabetic activities) of the extract. Therefore, UAE can be potentially used in combination with bio-based solvents, especially mixed VCO-PG, for maximizing bioactive phenolic isolation from MP. This study provided an alternative method for production of bio-based oil solution from MP which can be directly used as a functional ingredient in emulsion based food, neutraceutical and cosmetic products.