Multicomponent self nano emulsifying delivery systems of resveratrol with enhanced pharmacokinetics profile

Vasconcelos, Teófilo; Araújo, Francisca; Lopes, Carlos; Loureiro, Ana; Neves, José das; Marques, Sara; Sarmento, Bruno

doi:10.1016/j.ejps.2019.105011

Cited by 31 publications

(12 citation statements)

References 53 publications

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“…Efficacy of self-emulsification is also referred to as dispersability assessment [ 76 , 77 , 78 ]. Swift emulsification is considered highly favorable, if observed with SEDDSs intended for oral administration, as spontaneous emulsification is identified as the rate limiting step that must occur before successful absorption can ensue [ 78 ].…”

Section: Resultsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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A quality-by-design and characterization approach was followed to ensure development of self-emulsifying drug delivery systems (SEDDSs) destined for topical delivery of the highly lipophilic clofazimine. Solubility and water-titration experiments identified spontaneous emulsification capacity of different excipient combinations and clofazimine. After identifying self-emulsification regions, check-point formulations were selected within the self-emulsification region by considering characteristics required to achieve optimized topical drug delivery. Check-point formulations, able to withstand phase separation after 24 h at an ambient temperature, were subjected to characterization studies. Experiments involved droplet size evaluation; size distribution; zeta-potential; self-emulsification time and efficacy; viscosity and pH measurement; cloud point assessment; and thermodynamic stability studies. SEDDSs with favorable properties, i.e., topical drug delivery, were subjected to dermal diffusion studies. Successful in vitro topical clofazimine delivery was observed. Olive oil facilitated the highest topical delivery of clofazimine probably due to increased oleic acid levels that enhanced stratum corneum lipid disruption, followed by improved dermal clofazimine delivery. Finally, isothermal microcalometric experiments studied the compatibility of excipients. Potential interactions were depicted between argan oil and clofazimine as well as between Span®60 and argan-, macadamia- and olive oil, respectively. However, despite some mundane incompatibilities, successful development of topical SEDDSs achieved enhanced topical clofazimine delivery.

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Section: Resultsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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“…However, bioavailability is not optimal [4,46]. The use of nanocarriers to improve the bioavailability and maintain or improve the safety of RES is continuously explored to pursue its translation into clinical use [47,48]. Liposomes are known to be biocompatible; additionally, numerous studies show that liposomal entrapment can reduce the toxicity of incorporated compounds [49,50].…”

Section: Res Formulationmentioning

confidence: 99%

Toxicity Assessment of Resveratrol Liposomes-in-Hydrogel Delivery System by EpiVaginalTM Tissue Model

et al. 2022

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The natural polyphenol resveratrol (RES) has shown great potential as an antimicrobial, including against microbes associated with vaginal infections. To fully exploit the activities of RES, an all-natural ingredients formulation for RES delivery at vaginal site has been developed, namely liposomes loaded with RES, incorporated into a chitosan hydrogel as secondary vehicle. Although considered non-toxic and safe on their own, the compatibility of the final formulation must be evaluated for its biocompatibility and non-irritancy to the vaginal mucosa. As a preclinical safety assessment, the impact of RES formulation on the tissue viability, the effect on barrier function and cell monolayer integrity, and cytotoxicity were evaluated using the cell-based vaginal tissue model, the EpiVaginal™ tissue. RES liposomes-in-hydrogel formulations neither affected the mitochondrial activity, nor the integrity of the cell monolayer in RES concentration up to 60 µg/mL. Moreover, the barrier function was maintained to a greater extent by RES in formulation, emphasizing the benefits of the delivery system. Additionally, none of the tested formulations expressed an increase in lactate dehydrogenase activity compared to the non-treated tissues. The evaluation of the RES delivery system suggests that it is non-irritant and biocompatible with vaginal tissue in vitro in the RES concentrations considered as therapeutic.

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“…SMEDDS can be used as an excellent carrier for hydrophobic, poor absorbing and easily hydrolyzable drugs [19,20]. In recent years, SMEDDS has been extensively investigated for improving the oral bioavailability of unstable and water insoluble drugs, such as Ligusticum chuanxiong oil [21], curcumin [22], resveratrol [23] and simvastatin [24]. To the best of our knowledge, the formulation of phillygenin-loaded self-microemulsifying drug delivery system (PG-SMEDDS) has not been developed.…”

Section: Introductionmentioning

confidence: 99%

Self-Microemulsifying Drug Delivery System of Phillygenin: Formulation Development, Characterization and Pharmacokinetic Evaluation

et al. 2020

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Phillygenin, as an active ingredient of Forsythia suspensa, possesses a wide range of biological and pharmacological activity. However, its development and application are restricted due to its poor bioavailability and low solubility. Our work aimed to develop a self-microemulsifying drug delivery system to improve the oral bioavailability of phillygenin. The composition of the self-microemulsifying drug delivery system was preliminary screened by the pseudo-ternary phase diagram. Subsequently, the central composite design method was employed to optimize the prescription of the self-microemulsifying drug delivery system loaded with phillygenin. The prepared self-microemulsifying drug delivery system of phillygenin was characterized in terms of morphology, droplet size distribution, polydispersity index and stability. Then, the in vitro dissolution and the oral bioavailability were analyzed. The optimized self-microemulsifying drug delivery system of phillygenin consisted of 27.8% Labrafil M1944CS, 33.6% Cremophor EL, 38.6% polyethylene glycol 400 (PEG-400) and 10.2 mg/g phillygenin loading. The prepared self-microemulsifying drug delivery system of phillygenin exhibited spherical and uniform droplets with small size (40.11 ± 0.74 nm) and satisfactory stability. The in vitro dissolution experiment indicated that the cumulative dissolution rate of the self-microemulsifying drug delivery system of phillygenin was significantly better than that of free phillygenin. Furthermore, after oral administration in rats, the bioavailability of phillygenin was significantly enhanced by the self-microemulsifying drug delivery system. The relative bioavailability of the self-microemulsifying drug delivery system of phillygenin was 588.7% compared to the phillygenin suspension. These findings suggest that the self-microemulsifying drug delivery system of phillygenin can be a promising oral drug delivery system to improve the absorption of phillygenin.

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Multicomponent self nano emulsifying delivery systems of resveratrol with enhanced pharmacokinetics profile

Cited by 31 publications

References 53 publications

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Toxicity Assessment of Resveratrol Liposomes-in-Hydrogel Delivery System by EpiVaginalTM Tissue Model

Self-Microemulsifying Drug Delivery System of Phillygenin: Formulation Development, Characterization and Pharmacokinetic Evaluation

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