Almond oil O/W nanoemulsions: Potential application for ocular delivery

Hanieh, Patrizia Nadia; Bonaccorso, Angela; Zingale, Elide; Cimarelli, Silvia; Souto, Eliana B.; Rinaldi, Federica; Marianecci, Carlotta; Pignatello, Rosario; Carafa, Maria

doi:10.1016/j.jddst.2022.103424

Cited by 5 publications

(2 citation statements)

References 68 publications

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“…All SNEDDS showed pH values between 6.9 and 7.5 and osmolarity in the range of 0.281 to 0.320 Osm/kg after reconstitution with STF (1:10 by volume). These values could be considered optimal for an ophthalmic liquid formulation that should be non-irritating once applied [ 45 ]. Higher or lower values of osmolarity could cause irritation and extensive lachrymation, provoking a rapid wash-out of the solution and consequently a poor drug local bioavailability [ 46 ].…”

Section: Resultsmentioning

confidence: 99%

Formulating Resveratrol and Melatonin Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Ocular Administration Using Design of Experiments

Zingale,

Bonaccorso,

D’Amico

et al. 2024

Pharmaceutics

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Recent studies have demonstrated that Sirtuin-1 (SIRT-1)-activating molecules exert a protective role in degenerative ocular diseases. However, these molecules hardly reach the back of the eye due to poor solubility in aqueous environments and low bioavailability after topical application on the eye’s surface. Such hindrances, combined with stability issues, call for the need for innovative delivery strategies. Within this context, the development of self-nanoemulsifying drug delivery systems (SNEDDS) for SIRT-1 delivery can represent a promising approach. The aim of the work was to design and optimize SNEDDS for the ocular delivery of two natural SIRT-1 agonists, resveratrol (RSV) and melatonin (MEL), with potential implications for treating diabetic retinopathy. Pre-formulation studies were performed by a Design of Experiment (DoE) approach to construct the ternary phase diagram. The optimization phase was carried out using Response Surface Methodology (RSM). Four types of SNEDDS consisting of different surfactants (Tween® 80, Tween® 20, Solutol® HS15, and Cremophor® EL) were optimized to achieve the best physico-chemical parameters for ocular application. Stability tests indicated that SNEDDS produced with Tween® 80 was the formulation that best preserved the stability of molecules, and so it was, therefore, selected for further technological studies. The optimized formulation was prepared with Capryol® PGMC, Tween® 80, and Transcutol® P and loaded with RSV or MEL. The SNEDDS were evaluated for other parameters, such as the mean size (found to be ˂50 nm), size homogeneity (PDI < 0.2), emulsion time (around 40 s), transparency, drug content (>90%), mucoadhesion strength, in vitro drug release, pH and osmolarity, stability to dilution, and cloud point. Finally, an in vitro evaluation was performed on a rabbit corneal epithelial cell line (SIRC) to assess their cytocompatibility. The overall results suggest that SNEDDS can be used as promising nanocarriers for the ocular drug delivery of RSV and MEL.

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Section: Resultsmentioning

confidence: 99%

Formulating Resveratrol and Melatonin Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Ocular Administration Using Design of Experiments

Zingale,

Bonaccorso,

D’Amico

et al. 2024

Pharmaceutics

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“…On the other hand, Tween 20 enhanced mucoadhesive properties and diffusion into the mucus network of the eye compared to Tween 80 due to differences in charge and size. Both formulations formed stable nanoemulsions and showed no cytotoxic effect against Y-79 (human retinoblastoma cell line) cells [ 45 ].…”

Section: Topical Nano-formulations For Ocular Drug Deliverymentioning

confidence: 99%

Application of Convergent Science and Technology toward Ocular Disease Treatment

et al. 2023

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Eyes are one of the main critical organs of the body that provide our brain with the most information about the surrounding environment. Disturbance in the activity of this informational organ, resulting from different ocular diseases, could affect the quality of life, so finding appropriate methods for treating ocular disease has attracted lots of attention. This is especially due to the ineffectiveness of the conventional therapeutic method to deliver drugs into the interior parts of the eye, and the also presence of barriers such as tear film, blood-ocular, and blood-retina barriers. Recently, some novel techniques, such as different types of contact lenses, micro and nanoneedles and in situ gels, have been introduced which can overcome the previously mentioned barriers. These novel techniques could enhance the bioavailability of therapeutic components inside the eyes, deliver them to the posterior side of the eyes, release them in a controlled manner, and reduce the side effects of previous methods (such as eye drops). Accordingly, this review paper aims to summarize some of the evidence on the effectiveness of these new techniques for treating ocular disease, their preclinical and clinical progression, current limitations, and future perspectives.

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Nanoemulsion‐laden poly(vinyl) alcohol hydrogel films for transdermal delivery of carbamazepine

Rai,

Lakra,

Yadav

et al. 2024

Vinyl Additive Technology

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There is an unmet demand for transdermal devices that can deliver large dose of medications through the skin. Herein, nanoemulsion‐based poly(vinyl alcohol) (PVA) transdermal hydrogel films were developed for the high‐dose anti‐epileptic drug carbamazepine. A stable nanoemulsion was created with almond oil, Tween 60, and amphiphilic locust bean gum. The nanoemulsion had a hydrodynamic diameter of 251 nm, a polydispersity of 10.3%, and a zeta potential of −51.2 mV. Carbamazepine‐loaded nanoemulsion was blended with carbamazepine‐free PVA dispersion and casted into films. To accommodate a high dose, carbamazepine‐loaded nanoemulsion was trapped in a PVA dispersion containing carbamazepine to create transdermal films. The physicochemical characteristics and drug penetration characteristics of the produced films were compared. Both films had the uniform thickness, weight, and drug content. The folding endurance was found to be greater than 700 in both cases. Water vapor permeability decreased when carbamazepine was added to almond oil as well as polymer dispersion. FESEM pictures revealed a waxy paper‐like appearance for the PVA hydrogel film with dual drug‐reservoirs. FTIR spectra assessment revealed a hydrogen bonding interaction between PVA and carbamazepine. X‐ray diffraction examination revealed that the film contained an amorphous dispersion of carbamazepine. Dual carbamazepine reservoir‐based films outperformed single nanoemulsion drug reservoir‐based films in terms of drug flux through excised rat skin by 3.2 times. The in vitro skin permeation findings corresponded well to zero order kinetic models. Overall, this study showed that a high‐dose drug could be placed on nanoemulsion‐based transdermal PVA hydrogel films, resulting in improved skin permeability.Highlights Nanoemulsion was stable at almond oil:Tween 60/modified gum ratio of 5:5. Loading of high dose carbamazepine in nanoemulsion‐PVA transdermal films. Film of dual carbamazepine reservoir showed low water vapor permeation, moisture retention. Flux of carbamazepine from films improved three times through excised rat skin.

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Almond oil O/W nanoemulsions: Potential application for ocular delivery

Cited by 5 publications

References 68 publications

Formulating Resveratrol and Melatonin Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Ocular Administration Using Design of Experiments

Formulating Resveratrol and Melatonin Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Ocular Administration Using Design of Experiments

Application of Convergent Science and Technology toward Ocular Disease Treatment

Nanoemulsion‐laden poly(vinyl) alcohol hydrogel films for transdermal delivery of carbamazepine

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