Lipid-Based Nanoparticulate Systems for the Ocular Delivery of Bioactives with Anti-Inflammatory Properties.

The complexity of the eye structure and its physiology turned ocular drug administration into one of the most challenging topics in the pharmaceutical field. Ocular inflammation is one of the most common ophthalmic disorders. Topical administration of anti-inflammatory drugs is also commonly used as a side treatment in tissue repair and regeneration. The difficulty in overcoming the eye barriers, which are both physical and chemical, reduces drug bioavailability, and the frequency of administration must be increased to reach the therapeutic effect. However, this can cause serious side effects. Lipid nanoparticles seem to be a great alternative to ocular drug delivery as they are composed from natural excipients and can encapsulate both hydrophilic and lipophilic drugs of different sources, and their unique properties, as their excellent biocompatibility, safety and adhesion allow to increase the bioavailability, compliance and achieve a sustained drug release. They are also very stable, easy to produce and scale up, and can be lyophilized or sterilized with no significant alterations to the release profile and stability. Because of this, lipid nanoparticles show a great potential to be an essential part of the new therapeutic technologies in ophthalmology to deliver synthetic and natural anti-inflammatory drugs. In fact, there is an increasing interest in natural bioactives with anti-inflammatory activities, and the use of nanoparticles for their site-specific delivery. It is therefore expected that, in the near future, many more studies will promote the development of new nanomedicines resulting in clinical studies of new drugs formulations.

Factors Affecting the Retention Efficiency and Physicochemical Properties of Spray Dried Lipid Nanoparticles Loaded with Lippia sidoides Essential Oil.

Essential oils (EOs) are widely used in various industrial sectors but can present several instability problems when exposed to environmental factors. Encapsulation technologies are effective solutions to improve EOs properties and stability. Currently, the encapsulation in lipid nanoparticles has received significant attention, due to the several recognized advantages over conventional systems. The study aimed to investigate the influence of the lipid matrix composition and spray-drying process on the physicochemical properties of the lipid-based nanoparticles loaded with Lippia sidoides EO and their retention efficiency for the oil. The obtained spray-dried products were characterized by determination of flow properties (Carr Index: from 25.0% to 47.93%, and Hausner ratio: from 1.25 to 1.38), moisture (from 3.78% to 5.20%), water activity (<0.5), and powder morphology. Zeta potential, mean particle size and polydispersity index, of the redispersed dried product, fell between -25.9 mV and -30.9 mV, 525.3 nm and 1143 nm, and 0.425 and 0.652, respectively; showing slight differences with the results obtained prior to spray-drying (from -16.4 mV to -31.6 mV; 147 nm to 1531 nm; and 0.459 to 0.729). Thymol retention in the dried products was significantly lower than the values determined for the liquid formulations and was affected by the drying of nanoparticles.