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Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

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Nội dung chi tiết: Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity Aureli Calvct'.Luis J. del Valle1,2*, Jordi Puiggali1,2*1 Departament d’Enginyeria Química. Universitat Politècnica de Catalunya. Av. Diagonal 647.Ba

rcelona E-08028. Spain• Center for Research ill Nano-Engineering (Cr.NEt. Univcrsitat Politccnica de Catalunya. Edificic. C/Pasqual i Vila s/n. Barcel Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

ona E-08028. Spain*Corresponding author: LJ. del Valle (E-mail: luis.iavier.del.valle@upc.edu) and J.Puiggali (E-mail: Jọrdi.Puiggali@u{K.edu)ABSTRACT

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

Electrospraying of poly(butylene succinate) and its mixture with different indole derivatives was successfully performed using chloroform as solvent a

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activityy were dependent on the loaded drug and specifically on the type of substituent (methyl or phenyl) and its position in the indole core. In general, pa

rticles showed a raisin-like morphology caused by the shell collapsing of the resulting structurally weak microspheres. Accumulation of electrosprayed Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

panicles gave rise to consistent mats and they had a more hydrophobic surface than that determined for smooth films. The increase of hydrophobicity w

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

as mainly dependent on the porosity and the hydrophobic nature of the incorporated drugs. Indole derivatives were hardly delivered in a standard phosp

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activitys generally characterized by a fast burst effect and followed by establishment of an equilibrium condition that was dependent on the indole derivative

. However, a clearly different behavior was found when the indole was unable to form hydrogen bonds (c.g. 1-methylindole) since in this case a slow an Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

d sustained release was characteristic. Microspheres loaded with indole derivative showed a high antiproliferative activity that was dependent on enca

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

psulation efficiency and the type of loaded drug. The best results were specifically attained for the indole with an aromatic substituent. Interesting

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activityevention and treatment.Keywords: Elcctrospraying. pulyfbutylcne succinate), indole derivatives, drug release, anticancer activ ily.1.IntroductionElect

rospinning and elecuospraying arc elcctrohydrodynamic atomization techniques that arc widely employed in nanotechnology. These top-down physical metho Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

ds can lead Io materials at the nano- or microscale level tlnough the interaction between electrical energy and processed fluids |1,2| without involvi

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

ng a previous energy-transfer process (e.g. ultrasounds or microwaves) [3], Electrical energy from electrospinning allows the removal of organic solve

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activityon the application of a high voltage between the tip of a polymeric solution container and a counter electrode located at a collector. The solution dr

op at the tip is deformed by the electrical field, and when the electrostatic forces of repulsion overcome the droplet surface tension, a charged jet Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

ejecLS and deforms uniaxially through the electric field towards the collector. The microfluid jet is quickly dried (often in the order of 10 -seconds

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

) producing continuous nanosized fibers [7,8]. Loading of active substances such as drugs can also be easily achieved (e.g. by simple inclusion ol the

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activityn rales of p(M)rly-water soluble drugs. Therelore, electrospinning becomes a useful tool for generating solid dispersions of poorly water-soluble drug

s [9].The electrospray technique is derived from electrospinning. F.lectrosprayed particles are produced when the formed liquid jet undulates and brea Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

ks up into small electrically chaiged3droplets which repel each other and form a dispersed shower downwards to the collector. A progressive decrease i

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

n droplet diameter can be derived from the continuous evaporation of the solvent. Nowadays, electrospraying has grown in popularity because of its sim

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity electrospraying has been utilized to produce materials with a wide range of applications in areas as diverse as pharmaceutical, ceramics, cosmetics a

nd food industries but. especially, it appears useful for biomedical applications such as drug delivery [11].A great number of synthetic and natural p Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

olymers have been successfully formulated into microspheres by means of electrospraying [12-14]. Despite the simplicity of the process, operational pa

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

rameters must be experimentally found for each polymer in order to attain the desired particle size, morphology and size distribution.Biodegradable an

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activityomogeneous sizes for a good control of the drug release rate. Physicochemical properties of the selected polymer determine the interactions with the a

ctive compound and influence the drug encapsulation.'entrapment process as well as the drug release kinetics. Polylactides have been widely employed f Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

or encapsulation of therapeutic molecules due to their biodegradability and biocompatibility. Those requisites can also be found with polyfalkylen dic

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

arboxylate)s, being probably poly(butylene succinate) (PBS, Figure 1) the most significant polymer of this family-due to its unusual combination of go

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activityon [15].4Indole derivatives occur widely in natural products, existing in different kinds of plants, animals and marine organisms [16]. The indole cor

e is a near-ubiquitous component of biologically active natural products. For example, among the microorganisms in some bacteria, indole is used as a Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

cell-signaling molecule in both intra- and inter-species communication (process termed quorum sensing) [17,18]. The indole core is also well known as

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

one of the most important “scaffolds” for drug discovery, a term first introduced by Evans and co-workers to define scaffolds which are capable of ser

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activitytive compounds (Table 1). These possess certain biological features such as anticancer effectiveness [34-41] and antiviral activity [42]. Furthermore,

indole derivatives have the unique property of mimicking the structure of peptides and reversibly bind enzymes [43,44]. There is an amazing number of Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

approved indole containing drugs in the market as well as compounds currently going through different clinical phases or registration states. In fact

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

, seven indole-containing commercial drugs can be found between the Top-200 Best Selling Drugs by US Retail Sales in 2012 [45]. The most relevant is C

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity the broad spectrum and the important physiological activities of indole-derivatives make highly desirable the fabrication of loaded micro/nanopartide

s with them for their use in several biomedical applications. Herein, we report an efficient and simple strategy to prepare polybutylene succinate (PB Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

S) microspheres loaded with indole and indole-derivatives by means of the electrospraying technique. For this purpose, the effect of relevant processi

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

ng parameters (e.g. solvent, polymer concentration, applied voltage, tip-collector distance and flow rate) on the size and shape of the resulting micr

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: a system with anticancer activitySara K. Murase1, Mireia Aymat1.

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activityfferent positions of the ring (i.e. indole, 1-methylindole, 2-methylindole, 3-methylindole and 2-phenylindole) were evaluated. The comparison of these

five delivery systems was also performed, in terms of morphology, physicochemical properties, and biological activity, since it may provide an archet Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

ype model to understand encapsulation, release and stability from harsh environmental conditions for others compounds based on the indole ring.ITable

Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives a system with anticancer activity

1] [Fig. 1.12.Experimental section2.1.MaterialsPolybutylene succinate (PBS) is a commercial product (Bionollet 1001) supplied by Showa Denko K.K. (Ger

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