Enhanced pulmonary delivery of fluticasone propionate in rodents by mucus-penetrating nanoparticles

Попов, А. М.; Schopf, Lisa; Bourassa, James; Chen, Hongming

doi:10.1016/j.ijpharm.2016.02.031

Cited by 58 publications

(44 citation statements)

References 47 publications

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“…The key to designing and developing supersaturable formulations is to identify the optimal combination of "spring" and "parachute" [55,64]. Hence, the most common strategy to maintain supersaturation is to use PIs, such as polymers, surfactants, and/or cyclodextrins (CDs), which can act as both solubilization enhancers and PIs and can produce a combination of "spring" and "parachute" functions [34,65].…”

Section: Maintenance Of a Supersaturated State For The Improvement Ofmentioning

confidence: 99%

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Park

Kim

2020

Pharmaceutics

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Self-emulsifying drug delivery systems (SEDDSs) are a vital strategy to enhance the bioavailability (BA) of formulations of poorly water-soluble compounds. However, these formulations have certain limitations, including in vivo drug precipitation, poor in vitro in vivo correlation due to a lack of predictive in vitro tests, issues in handling of liquid formulation, and physico-chemical instability of drug and/or vehicle components. To overcome these limitations, which restrict the potential usage of such systems, the supersaturable SEDDSs (su-SEDDSs) have gained attention based on the fact that the inclusion of precipitation inhibitors (PIs) within SEDDSs helps maintain drug supersaturation after dispersion and digestion in the gastrointestinal tract. This improves the BA of drugs and reduces the variability of exposure. In addition, the formulation of solid su-SEDDSs has helped to overcome disadvantages of liquid or capsule dosage form. This review article discusses, in detail, the current status of su-SEDDSs that overcome the limitations of conventional SEDDSs. It discusses the definition and range of su-SEDDSs, the principle mechanisms underlying precipitation inhibition and enhanced in vivo absorption, drug application cases, biorelevance in vitro digestion models, and the development of liquid su-SEDDSs to solid dosage forms. This review also describes the effects of various physiological factors and the potential interactions between PIs and lipid, lipase or lipid digested products on the in vivo performance of su-SEDDSs. In particular, several considerations relating to the properties of PIs are discussed from various perspectives.Pharmaceutics 2020, 12, 365 2 of 57 intraluminal supersaturation and the biorelevance of supersaturation assays will be addressed. Finally, we will make suggestions for the successful development of su-SEDDs.There are many review articles that give useful information about the nature and application of supersaturable drug delivery systems or conventional SEDDSs. However, these reviews cover only a limited range of su-SEDDSs. Therefore, this review, which includes the current status of technology focused only on su-SEDDSs, is a valuable addition to the previous review literature because no review article currently covers such a wide range of su-SEDDSs. Conventional Solubilized SEDDSsThere has been a steady increase in the number of new drug candidates (almost 40%) that are highly hydrophobic and poorly water-soluble. The oral bioavailability of poorly water-soluble drugs is hindered by low solubility and slow dissolution in the aqueous environment of the GIT. Thus, it is a great challenge for pharmaceutical scientists to overcome the inherent slow dissolution and poor oral absorption of hydrophobic drugs [1][2][3][4]. SEDDSs have emerged as a promising approach to improving the biopharmaceutical performance of hydrophobic drugs by enhancing their bioavailability [5,6].An SEDDS is a pre-concentrate composed of a drug, oils, surfactants, and sometimes co-solvents and/or co-surfactan...

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Section: Maintenance Of a Supersaturated State For The Improvement Ofmentioning

confidence: 99%

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Park

Kim

2020

Pharmaceutics

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“…Some of the research works undertaken during the last years have proposed the vectorization in nanoparticles, via nanoprecipitation, of hydrophobic active molecules, mainly exhibiting logP values higher than 3. They include antineoplastics (e.g., doxorubicin [4], paclitaxel [5,6], docetaxel [7,8], methotrexate [9], triptolide [6], cucurbitacin [10], and sorafenib [11]), antiretrovirals (e.g., efavirenz [12] and nevirapine [13]), immune suppressants (mycophenolate [14]), anti-inflammatories (clobetasol [15], fluticasone propionate [16], dexamethasone [17,18], and diclofenac [19]), antimicrobial and antifungal agents (polymyxin B [20], amphotericin B [21], itraconazole [22], and linezolid [23]), antihyperlipidemics (fenofibrate [24,25]), anesthetics (tetracaine [26] and ketamine [27]), antihypertensives (nimodipine [28] and atenolol [29]), vitamins or their precursors (β-carotene [30] and vitamin E [31]), and antioxidants (quercetin [14,32]). Likewise, although in a much smaller number, hydrophilic active molecules such alendronate [33], N-acetylcysteine [34], and calcein [35], have been investigated.…”

Section: Introductionmentioning

confidence: 99%

Nanoprecipitation: Applications for Entrapping Active Molecules of Interest in Pharmaceutics

Martínez-Muñoz¹,

Ospina-Giraldo²,

Mora-Huertas³

2021

Nano- And Microencapsulation - Techniques and Applications

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Nanoprecipitation technique, also named solvent injection, spontaneous emulsification, solvent displacement, solvent diffusion, interfacial deposition, mixinginduced nanoprecipitation, or flash nanoprecipitation, is recognized as a useful and versatile strategy for trapping active molecules on the submicron and nanoscale levels. Thus, these particles could be intended among others, for developing innovative pharmaceutical products bearing advantages as controlled drug release, target therapeutic performance, or improved stability and organoleptic properties. On this basis, this chapter offers readers a comprehensive revision of the state of the art in research on carriers to be used for pharmaceutical applications and developed by the nanoprecipitation method. In this sense, the starting materials, the particle characteristics, and the in vitro and in vivo performances of the most representative of these carriers, i.e., polymer, lipid, and hybrid particles have been analyzed in a comparative way searching for a general view of the obtained behaviors.

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“…As for other therapies, especially for chronic diseases, drug administration directly to the lungs, instead of oral or parenteral administrations, allows using lower doses to obtain an equivalent therapeutic response, reducing several side effects, and the toxicity of the drugs. For many of them, however, the therapeutic efficacy after inhalation is often reduced due to the fast clearance from the lung, being rapidly adsorbed and, thus, reaching the circulatory system [ 4 ]. Therefore, in order to increase the pulmonary efficacy of FP and to modulate the drug release profile, an innovative strategy could be adopted in order to prolong the FP residence time in the lung, that is, the entrapment of the drug into colloidal drug delivery systems and their administration as an aerosolized formulation [ 2 ].…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, in order to increase the pulmonary efficacy of FP and to modulate the drug release profile, an innovative strategy could be adopted in order to prolong the FP residence time in the lung, that is, the entrapment of the drug into colloidal drug delivery systems and their administration as an aerosolized formulation [ 2 ]. Moreover, a further goal is to maximize lung residence time; mucus-penetrating particles must also be designed by realizing nanoparticles possessing a coating specifically able to minimize adhesive interactions with mucin fibers, thus penetrating readily into the pulmonary mucus layer [ 4 , 5 , 6 ]. In particular, this strategy could be targeted by the attachment of hydrophilic uncharged polymers, like polyethylenglycol (PEG) to drugs, proteins, and particles, which seems to reduce interactions with sialic acid, a major component of mucus [ 7 , 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

“…In particular, this strategy could be targeted by the attachment of hydrophilic uncharged polymers, like polyethylenglycol (PEG) to drugs, proteins, and particles, which seems to reduce interactions with sialic acid, a major component of mucus [ 7 , 8 , 9 ]. Recently, Popov and coworkers [ 4 ] realized FP-loaded mucus-penetrating nanoparticles and, by in vivo experiments, demonstrated that the pulmonary administration achieved a higher local exposure to FP in lungs of rodents when compared to free drug, leading to a significant extension of the anti-inflammatory effect of FP in a rat lung inflammation model as compared to a non-encapsulated FP control.…”

Section: Introductionmentioning

confidence: 99%

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Polyaspartamide-Based Nanoparticles Loaded with Fluticasone Propionate and the In Vitro Evaluation towards Cigarette Smoke Effects

et al. 2017

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This paper describes the evaluation of polymeric nanoparticles (NPs) as a potential carrier for lung administration of fluticasone propionate (FP). The chosen polymeric material to produce NPs was a copolymer based on α,β-poly(N-2-hydroxyethyl)-d,l-aspartamide (PHEA) whose backbone was derivatised with different molecules, such as poly(lactic acid) (PLA) and polyethylenglycol (PEG). The chosen method to produce NPs from PHEA-PLA-PEG2000 was the method based on high-pressure homogenization and subsequent solvent evaporation by adding Pluronic F68 during the process and trehalose before lyophilisation. Obtained colloidal FP-loaded NPs showed a slightly negative surface charge and nanometric dimensions that are maintained after storage for one year at −20 °C and 5 °C. The FP loading was about 2.9 wt % and the drug was slowly released in simulated lung fluid. Moreover, the obtained NPs, containing the drug or not, were biocompatible and did not induce cell necrosis and cell apoptosis on bronchial epithelial cells (16-HBE). Further in vitro testing on cigarette smoke extract (CSE)-stimulated 16-HBE revealed that FP-loaded NPs were able to reduce the survivin expression, while either free FP or empty NPs were not able to significantly reduce this effect.

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Enhanced pulmonary delivery of fluticasone propionate in rodents by mucus-penetrating nanoparticles

Cited by 58 publications

References 47 publications

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Nanoprecipitation: Applications for Entrapping Active Molecules of Interest in Pharmaceutics

Polyaspartamide-Based Nanoparticles Loaded with Fluticasone Propionate and the In Vitro Evaluation towards Cigarette Smoke Effects

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