Microemulsions are widely studied as potential ocular drug delivery vehicles. In the present study we show the versatility of possible use microemulsions as ocular delivery vehicle. The ME is loaded with a hydrophilic drug, riboflavin phosphate (RFP) and a lipophilic, docosahexaenoic acid in triglyceride form (TG-DHA), each sep. These drugs treat keratoconus and dry eye syndrome, resp. The advantage of using ME loaded with RFP is in overcoming eye epithelium debridement during collagen crosslinking therapy for treatment of keratoconus. ME loaded with lipophilic TG-DHA provides convenient dosage in liq. aq. form of administration of highly lipophilic TG-DHA, which is known as a protective mol. in dry eye syndrome. The capability of RFP-loaded MEs was demonstrated in terms of improvement of biomech. strength of the rabbit cornea, as a result of successful penetration of RFP through the intact epithelium. TG-DHA-loaded microemulsion applied topically onto an eye with induced dry eye syndrome showed the significant relief of the dry eye condition. [on SciFinder(R)]

Microemulsions (MEs) have gained increasing interest as carriers of hydrophobic bioactives in the last decades. However, it is still difficult to control the uptake and the release of bioactives directly extd. from plants. In this study, modified ME nanodroplets (nano-sized self-assembled liqs., NSSLs) were employed as extn. medium of gossypol, a toxic component of cottonseed. Loading was performed using both pure gossypol, and gossypol obtained by extn. from cottonseed. We achieved two goals: (i) remove gossypol from cottonseed to obtain cotton-oil free of gossypol; and (ii) ext. gossypol directly into a nano-delivery vehicle for biomedical purposes. Structural and dynamical information on the unloaded and gossypol-loaded NSSL systems were obtained by self-diffusion NMR, SD-NMR, and spin-probe ESR (EPR) studies. The results showed that NSSL formed fluid water-in-oil (W/O) nano domains at the lowest water contents; a more viscous bicontinuous structure at comparable oil and water contents, and, finally, oil-in-water (O/W, micellar-like) at the higher concn. of water. These micellar-like structures were more fluid at the external hydrated surface, as demonstrated by SD-NMR, while the lipidic region tested by EPR revealed an increasing packing. In all these structures, gossypol mainly localized in the lipophilic region close to the water interface. Overall, SD-NMR and EPR provided complementary information, helping to clarify the structural properties of NSSLs formed at different water contents and their ability to incorporate gossypol also directly from cottonseed-NSSL mixts. [on SciFinder(R)]

The present disclosure provides cannabinoid-loaded formulations, as well as processes for their prepn. [on SciFinder(R)]

The disclosure concerns viscous or gelled delivery systems based on oily nano-domains dispersed in a viscosified/gelled continuous aq. phase, and suitable for prolonged and/or sustained topical delivery of various active compds. [on SciFinder(R)]

The present disclosure provides methods for extn. of various agents, e.g. active agent, from a plant source, specifically with the use of extn. formulations which are based on micellar liq. systems. [on SciFinder(R)]

The present disclosure provides methods for selective extn. of cannabinoids, for example cannabidiol (CBD), from a plant source, by using tailored extn. media. [on SciFinder(R)]

In the present study we aimed to control insulin release from the reverse hexagonal (H-II) mesophase using Thermomyces lanuginosa lipase (TLL) in the environment (outer TLL) or within the H-II cylinders (inner TLL). Two insulin-loaded systems differing by the presence (or absence) of phosphatidylcholine (PC) were examined. In general, incorporation of PC into the H-II interface (without TLL) increased insulin release, as a more cooperative system was formed. Addition of TLL to the systems' environments resulted in lipolysis of the H-II structure. In the absence of PC, the lipolysis was more dominant and led to a significant increase in insulin release (50% after 8 h). However, the presence of PC stabilized the interface, hindering the lipolysis, and therefore no impact on the release profile was detected during the first 8 h. Entrapment of TLL within the H-II cylinders (with and without PC) drastically increased insulin release in both systems up to 100%. In the presence of PC insulin released faster and the structure was more stable. Consequently, the presence of lipases (inner or outer) both enhanced the destruction of the carrier, and provided sustained release of the entrapped insulin. (C) 2017 Elsevier B.V. All rights reserved.

The present invention concerns novel dilutable delivery systems and propofol microemulsions suitable for i.v. delivery of propofol. [on SciFinder(R)]

The present work reports on the prepn. and characterization of progesterone-loaded reverse hexagonal (HII) mesophase based on a glycerol monooleate (GMO)/tricaprylin (TAG)/water mixt. for transdermal application. Several compns. into which progesterone was quant. solubilized were selected and used in the present study in order to evaluate the effect of the hormone on structural transitions and characteristics. A GMO/TAG of 90:1 wt ratio with 20 wt% water was found to form HII mesophases with relative high solubilization capacity of 4 wt% progesterone and a shelf life of over one year. The structures were identified by cross-polarized light microscopy (CPLM). Structural confirmations were obtained from small-angle X-ray scattering (SAXS) measurements. The hormone is solubilized at the interface of the HII mesophase as confirmed by SAXS, rheol., FTIR, and DSC. The progesterone, which is loaded onto reverse hexagonal cylinders, leads to strengthening the hydrogen bonding and to better packing of the HII mesophase, suggesting that progesterone is a kosmotropic agent. The reverse hexagonal mesophase seems to be a promising carrier for solubilization of progesterone. [on SciFinder(R)]