Self-emulsifying drug delivery systems: Design of a novel vaginal delivery system for curcumin

Köllner, S.; Nardin, Isabelle; Markt, Rudolf; Griesser, Janine; Prüfert, Felix; Bernkop‐Schnürch, Andreas

doi:10.1016/j.ejpb.2017.03.012

Cited by 39 publications

(22 citation statements)

References 21 publications

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“…Despite curcumin's therapeutic benefits, translation of doses for clinical application is unfeasible due to its poor bioavailability contributed by poor solubility (<1 mg/ml), slow dissolution rate, extensive intestinal and hepatic metabolic transformation along with its rapid elimination [11,12]. So far, literature reports development of various drug delivery systems like liposomes [13,14], cyclodextrin complexes [15], self-emulsifying system [16,17], biodegradable polymeric nanoparticles [18,19], solid lipid nanoparticles (SLNs) [20,21], nano-emulsion [22,23] for topical and parenteral delivery of curcumin in variety of therapeutic applications. However, curcumin formulations have conferred confined success via oral route.…”

Section: Introductionmentioning

confidence: 99%

Improved uptake and therapeutic intervention of curcumin via designing binary lipid nanoparticulate formulation for oral delivery in inflammatory bowel disorder

Sharma

Wadhwa

2019

Artificial Cells, Nanomedicine, and Biotechnology

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This study was focussed on development of curcumin loaded solid binary lipid nanoparticles (C-SBLNs) to ameliorate stability, uptake and therapeutic potential of curcumin during inflammatory bowel disease (IBD). C-SBLNs with nano-size range (210.56 ± 41.22 nm) and high entrapment efficiency (83.12 ± 6.57%) were prepared by solvent emulsification evaporation method using binary lipids i.e. stearic acid and tristearin after optimizing various formulation and process variables. Physicochemical characterization of C-SBLNs by ATR-FTIR confirmed drug entrapment whereas thermal and pXRD study corroborated loss of crystallinity of drug into C-SBLNs. Lyophilized C-SBLNs were found to be spherical shaped with good gastrointestinal stability and prolonged drug release up to 24 h. Optimized C-SBLNs formulation displayed significantly enhanced cellular uptake and localization in inflamed tissues during IBD. Oral administration of C-SBLNs in DSS induced colitis model revealed significant reduction in leucocyte infiltration, oxidative stress, pro-inflammatory cytokine (TNF-a) secretion and maintenance of colonic structure similar to healthy animal group compared to curcumin. Thus, in vitro and preclinical findings of study clearly confirmed that C-SBLNs could be a stable and efficacious alternative platform for curcumin delivery with strong competence in IBD chemotherapy.

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Section: Introductionmentioning

confidence: 99%

Improved uptake and therapeutic intervention of curcumin via designing binary lipid nanoparticulate formulation for oral delivery in inflammatory bowel disorder

Sharma

Wadhwa

2019

Artificial Cells, Nanomedicine, and Biotechnology

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“…The initial oral SEDDSs can transform the lipid-based drug delivery of hydrophobic drugs via the topical/transdermal route. This statement is supported by successful drug deliveries achieved by SEDDSs developed to improve drug delivery via alternative topical administration routes such as the ocular-, rectal-, vaginal-, and nasal routes of administration [19][20][21][22][23][24][25]. Moreover, SEDDSs remain noteworthy drug delivery vehicles, since approximately 30% of current drugs on the commercial market, together with up to 50% of newly discovered drugs, are of a noteworthy lipophilic nature [17,[48][49][50][51].…”

Section: Discussionmentioning

confidence: 94%

“…Despite the fact that the literature cannot provide a clear explanation for the mechanism of spontaneous emulsification, the evident success of the self-emulsification drug delivery approach cannot be denied [19][20][21][22][23][24][25]32,33]. Additionally, pseudo-ternary-phase diagrams assist in predicting the behaviours of emulsions established by mysterious spontaneous emulsification [33,100].…”

Section: Discussionmentioning

confidence: 99%

“…However, numerous solidification techniques have been explored, such as transforming liquid SEDDSs into pellets, dispersible powders, and granules, in order to improve stability of these uniquely simplified systems [2,15,18]. Moreover, apart from rendering enhanced oral drug delivery, SEDDSs have demonstrated the potential for improving drug delivery via diverse pathways, including the ocular-, vaginal-, rectal-, and nasal routes of administration [19][20][21][22][23][24][25]. For example, a recent study was published as the first proof of concept for employing SEDDSs as an oral vaccination vehicle.…”

Section: Introductionmentioning

confidence: 99%

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Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

2020

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Self-emulsifying drug delivery systems (SEDDSs) originated as an oral lipid-based drug delivery system with the sole purpose of improving delivery of highly lipophilic drugs. However, the revolutionary drug delivery possibilities presented by these uniquely simplified systems in terms of muco-adhesiveness and zeta-potential changing capacity lead the way forward to ground-breaking research. Contrarily, SEDDSs destined for topical/transdermal drug delivery have received limited attention. Therefore, this review is focused at utilising principles, established during development of oral SEDDSs, and tailoring them to fit evaluation strategies for an optimised topical/transdermal drug delivery vehicle. This includes a detailed discussion of how the authentic pseudo-ternary phase diagram is employed to predict phase behaviour to find the self-emulsification region most suitable for formulating topical/transdermal SEDDSs. Additionally, special attention is given to the manner of characterising oral SEDDSs compared to topical/transdermal SEDDSs, since absorption within the gastrointestinal tract and the multi-layered nature of the skin are two completely diverse drug delivery territories. Despite the advantages of the topical/transdermal drug administration route, certain challenges such as the relatively undiscovered field of skin metabolomics as well as the obstacles of choosing excipients wisely to establish skin penetration enhancement might prevail. Therefore, development of topical/transdermal SEDDSs might be more complicated than expected.

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“…This study also showed that SEDDS with a smaller particle size (25 nm) and most negatively charged (zeta potential -25 mV) is the most effective muco-diffusive compared with other SEDDS [58]. The Transwell method was utilized to understand the influence of papain on the mucus diffusion of a SEDDS [124]; to understand the mucus penetration profiles of phosphorylated zeta potential changing SEDDS [130]; and for the determination of the permeation potential of curcumin loaded into SEDDS [148].…”

Section: Transwell Chamber Techniquesmentioning

confidence: 95%

Self-emulsifying drug delivery system: Mucus permeation and innovative quantification technologies

Abdulkarim

Sharma

Gumbleton

2019

Advanced Drug Delivery Reviews

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Mucus is a dynamic barrier which covers and protects the underlying mucosal epithelial membrane against bacteria and foreign particles. This protection mechanism extends to include therapeutic macromolecules and nanoparticles (NPs) through trapping of these particles. Mucus is not only a physical barrier that limiting particles movements based on their sizes but it selectively binds with particles through both hydrophilic and lipophilic interactions. Therefore, nano-carriers for mucosal delivery should be designed to eliminate entrapment by the mucus barrier. For this reason, different strategies have been approached for both solid nano-carriers and liquid core nano-carriers to synthesise muco-diffusive nano-carrier. Among these nano-strategies, Self-Emulsifying Drug Delivery System (SEDDS) was recognised as very promising nano-carrier for mucus delivery. The system was introduced to enhance the dissolution and bioavailability of orally administered insoluble drugs. SEDDS has shown high stability against intestinal enzymatic activity and more importantly, relatively rapid permeation characteristics across mucus barrier. The high diffusivity of SEDDS has been tested using various in vitro measurement techniques including both bulk and individual measurement of droplets diffusion within mucus. The selection and processing of an optimum in vitro technique is of great importance to avoid misinterpretation of the diffusivity of SEDDS through mucus barrier. In conclusion, SEDDS is a system with high capacity to diffuse through intestinal mucus even though this system has not been studied to the same extent as solid nano-carriers.

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Self-emulsifying drug delivery systems: Design of a novel vaginal delivery system for curcumin

Cited by 39 publications

References 21 publications

Improved uptake and therapeutic intervention of curcumin via designing binary lipid nanoparticulate formulation for oral delivery in inflammatory bowel disorder

Improved uptake and therapeutic intervention of curcumin via designing binary lipid nanoparticulate formulation for oral delivery in inflammatory bowel disorder

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

Self-emulsifying drug delivery system: Mucus permeation and innovative quantification technologies

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