Oral films as breakthrough tools for oral delivery of proteins/peptides

Castro, Pedro M.; Fonte, Pedro; Sousa, Flávia; Madureira, Ana Raquel; Sarmento, Bruno; Pintado, Manuela

doi:10.1016/j.jconrel.2015.05.258

Cited by 52 publications

(23 citation statements)

References 107 publications

(99 reference statements)

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“…Moreover, when nanoparticles are produced as buccal delivery systems, the polymers must be mucoadhesive to increase the residence time of the delivery system, enhancing the drug uptake and the amount that reaches the systemic circulation [123]. The mucoadhesion is mostly obtained either by the formation of electrostatic interactions, and by the formation of hydrogen bonds with the mucus layer.…”

Section: Polymer Nanoparticlesmentioning

confidence: 99%

Novel and revisited approaches in nanoparticle systems for buccal drug delivery

Macedo

Castro

Roque

et al. 2020

Journal of Controlled Release

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106

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The buccal route is considered patient friendly due to its non-invasive nature and ease of administration. Such delivery route has been used as an alternative for the delivery of drugs that undergo first-pass metabolism or are susceptible to pH and enzymatic degradation, such as occurs in the gastrointestinal tract. However, the drug concentration absorbed in the buccal mucosa is often low to obtain an acceptable therapeutic effect, mainly due to the saliva turnover, tongue and masticatory movements, phonation, enzymatic degradation and lack of epithelium permeation.Therefore, the encapsulation of drugs into nanoparticles is an important strategy to avoid such problems and improve their buccal delivery. Different materials from lipids to natural or synthetic polymers and others have been used to protect and deliver drugs in a sustained, controlled or targeted manner, and enhance their uptake through the buccal mucosa improving their bioavailability and therapeutic outcome. Overall, the main aim of this review is to perform an overview about the nanotechnological approaches developed so far to improve the buccal delivery of drugs. Herein, several types of nanoparticles and delivery strategies are addressed, and a special focus on pipeline products is also given.

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Section: Polymer Nanoparticlesmentioning

confidence: 99%

Novel and revisited approaches in nanoparticle systems for buccal drug delivery

Macedo

Castro

Roque

et al. 2020

Journal of Controlled Release

Self Cite

106

View full text Add to dashboard Cite

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“…Other properties like the antibacterial activity of chitosan and polycarbophil have also been exploited to eliminate bacteria that are prone to degrade sensitive molecules [17].…”

Section: Physical Modifications Of Fp To Enhance Oral Bioavailabilitymentioning

confidence: 99%

“…Nevertheless, the small size and form of the oral films have limited their incorporating capacities as active molecules; thus, they must be potent enough at low doses [17].…”

Section: Fp Solid Particles Systems As Enhancement Alternative Of Senmentioning

confidence: 99%

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Functionalized Polymers for Enhance Oral Bioavailability of Sensitive Molecules

et al. 2016

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Currently, many sensitive molecules have been studied for effective oral administration. These substances are biologically active compounds that mainly suffer early degradation in the gastrointestinal tract (GIT) and physicochemical instability, inactivation and poor solubility and permeability. The sensibility of the biomolecules has limited their oral administration in the body and today is an important research topic to achieve desired effects in medicine field. Under this perspective, various enhancement approaches have been studied as alternatives to increase their oral bioavailability. Some of these strategies include functionalized polymers to provide specific useful benefits as protection to the intestinal tract by preventing its degradation by stomach enzymes, to increase their absorption, permeability, stability, and to make a proper release in the GIT. Due to specific chemical groups, shapes and sizes, morphologies, mechanical properties, and degradation, recent advances in functionalized polymers have opened the door to great possibilities to improve the physicochemical characteristics of these biopharmaceuticals. Today, many biomolecules are found in basic studies, preclinical steps, and others are late stage clinical development. This review summarizes the contribution of functionalized polymers to enhance oral bioavailability of sensitive molecules and their application status in medicine for different diseases. Future trends of these polymers and their possible uses to achieve different formulation goals for oral delivery are also covered in this manuscript.

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“…[1][2][3][4][5] Besides all the advantages of the oral route, factors like low aqueous solubility of drugs, limited gastrointestinal (GI) absorption, rapid metabolism of drug, and low mucosal permeability play a major role in the disappointing in vivo results. [5][6][7][8] The intestinal mucosa plays an effective role as a physical barrier that covers the surfaces of the GI tract, allowing selective absorption of nutrients, electrolytes, and fluids, at the same time protecting the host from environmental pathogens.…”

Section: Introductionmentioning

confidence: 99%

Design and statistical modeling of mannose-decorated dapsone-containing nanoparticles as a strategy of targeting intestinal M-cells

Vieira¹,

Chaves²,

Pinheiro³

et al. 2016

IJN

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The aim of the present work was to develop and optimize surface-functionalized solid lipid nanoparticles (SLNs) for improvement of the therapeutic index of dapsone (DAP), with the application of a design of experiments. The formulation was designed to target intestinal microfold (M-cells) as a strategy to increase internalization of the drug by the infected macrophages. DAP-loaded SLNs and mannosylated SLNs (M-SLNs) were successfully developed by hot ultrasonication method employing a three-level, three-factor Box–Behnken design, after the preformulation study was carried out with different lipids. All the formulations were systematically characterized regarding their diameter, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency, and loading capacity. They were also subjected to morphological studies using transmission electron microscopy, in vitro release study, infrared analysis (Fourier transform infrared spectroscopy), calorimetry studies (differential scanning calorimetry), and stability studies. The diameter of SLNs, SLN-DAP, M-SLNs, and M-SLN-DAP was approximately 300 nm and the obtained PDI was <0.2, confirming uniform populations. Entrapment efficiency and loading capacity were approximately 50% and 12%, respectively. Transmission electron microscopy showed spherical shape and nonaggregated nanoparticles. Fourier transform infrared spectroscopy was used to confirm the success of mannose coating process though Schiff’s base formation. The variation of the ZP between uncoated (approximately −30 mV) and mannosylated formulations (approximately +60 mV) also confirmed the successful coating process. A decrease in the enthalpy and broadening of the lipid melting peaks of the differential scanning calorimetry thermograms are consistent with the nanostructure of the SLNs. Moreover, the drug release was pH-sensitive, with a faster drug release at acidic pH than at neutral pH. Storage stability for the formulations for at least 8 weeks is expected, since they maintain the original characteristics of diameter, PDI, and ZP. These results pose a strong argument that the developed formulations can be explored as a promising carrier for treating leprosy with an innovative approach to target DAP directly to M-cells.

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Oral films as breakthrough tools for oral delivery of proteins/peptides

Cited by 52 publications

References 107 publications

Novel and revisited approaches in nanoparticle systems for buccal drug delivery

Novel and revisited approaches in nanoparticle systems for buccal drug delivery

Functionalized Polymers for Enhance Oral Bioavailability of Sensitive Molecules

Design and statistical modeling of mannose-decorated dapsone-containing nanoparticles as a strategy of targeting intestinal M-cells

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