INFLUENCE OF MCM-41 PARTICLES MORPHOLOGY AND FUNCTIONALIZATION ON IBUPROFEN UPTAKE AND RELEASE VI Convegno Nazionale sulla Scienza e Tecnologia dei Materiali

INFLUENCE OF MCM-41 PARTICLES MORPHOLOGY AND FUNCTIONALIZATION ON

IBUPROFEN UPTAKE AND RELEASE

VI Convegno Nazionale sulla Scienza e Tecnologia dei Materiali. Perugia 12-15 giugno 2007

Valentina Aina

1. V. Aina, G. Cerrato, G. Magnacca, C. MorterraDip. Chimica IFM, Università di Torino, Torino-Italy

2. V. Cauda, B. Onida, E. GarroneDip. di Scienza dei Materiali e Ingegneria Chimica Politecnico di Torino, Torino-Italy

3. F. Balas, M. Colilla, M. Manzano, M. Vallet-RegìDpto. de Quimica Inorganica y Bioinorganica Universidad Complutense de Madrid, Madrid-Spain

4. M. Rodriguez, C. OteroDpto de Quimica, Universidad de las Islas Baleares, Palma de Mallorca-Spain

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Particles morphology influence for drug release

Irregular particlesSpherical particles

Functionalization influence for drug release

SiSi

OHOH

OHSi

Ordered mesoporous silica: MCM-41Ordered mesoporous silica: MCM-41

Ordered mesoporous silica allow to adsorb and deliver a drug in a homogeneous and

controlled way



2 m 2 m 2 m

(a) (b) (c)

2 m2 m 2 m2 m 2 m2 m

(a) (b) (c)

Sphericals particles

490 nm 615 nm 770 nm

Name samples Description

MCM-41 irr MCM-41 particles of irregular shape

MCM-41 sph. 490 nm MCM-41 particles of spherical shape, with dimension of 490 nm



Irregulares particles

SEMSEM



SamplesDp

(nm) Vp

(cm3/g)SBET

(m2/g)

MCM-41 sph 490nm 2,1 0,46 874

MCM-41 sph 615nm 1,78 0,48 1078

MCM-41 sph 770nm 1,95 0,58 1198

SamplesDp

(nm) Vp

(cm3/g)SBET

(m2/g)

MCM-41 IRR 3,4 0,80 928

Samples characterizationSamples characterization



[drug]mesoporous [drug]solvent

Uptake conditions: mg ibuprofen/ mg material = 1 Solution of ibuprofen with n-pentane (33 mg/ml) 24h with stirring (two methods):

- magnetic stirring- orbital stirring

mesoporous material

drug solution

Samples% ibuprofen (TGA/DTA)

MCM-41 Irr+ Ibu 21%

MCM-41 sph 490 nm + Ibu 11%



Samples% ibuprofen (TGA/DTA)

MCM-41 Irr+ Ibu 26%




Magnetic stirring Orbital stirring

Ibuprofen UptakeIbuprofen Uptake



2.5 nm

SamplesDp

(nm) Vp

(cm3/g)SBET

(m2/g)

MCM-41 IRR 3,4 0,80 928

MCM-41 IRR + Ibu 2,5 0,32 514

MCM-41 IRR after release ibu / 0,33 134


mesoporous material +

drug

Release conditions

Samples Simulated biological fluids (SBF) at 37ºC and pH 7,4 Continuos stirring 50 mg of samples with 14 ml of SBF Ibuprofen released monitored with UV-Vis

Ibuprofen releaseIbuprofen release

SBF solution




Release fast 80% of ibuprofen released during the first 9 hours 15% of ibuprofen released more slowly Spherical particles release the drug more slowly then irregular particles Smaller are the spherical particles, slower is the ibuprofen release



R

The aim is to integrate organic groups onto the pores surface through Si-C covalent bonds, oriented towards the inner axes of the channels.

Functionalized mesoporous materials Functionalized mesoporous materials

High degree of functionalization

Homogeneous distribution throughout the pores surface

To preserve the mesoporous structural arrangement due to its significance in future applications

Requisites


Si

Si

OH

Si OSiNH2

NH2

OSiSi

Si

Si

OSiSi

Si

Si

OSiSi

Si

HO

Si

SiO

SiO

Si

Si

Si

Si

Si

Si

Si

Si

HO

Si

SiO

SiO Si

Si

Si

Si

Si

Si

SiSi

OHSi

CH3CH3

OSiSiO

SiSi

Si

3

SiSi

Si

Si

SiOH

Si

Cl

SiO

Cl

SiO

Si

Si

Si Si

Si

Si

Si

SiOH

Si

OSi

CN

OSi

CN

Si

Si

Si

N

Si

Si

Si

OHOH HOSi

SiSi

SiSi

SiSiSi

Si

Si

OH

Si

SHOSi

SHOSi

Si

Si

OH

OSi

Si

Si

Si

Functionalization vs ibuprofen interactionFunctionalization vs ibuprofen interaction

MCM-41 functionalization with AP-TES:

to investigate the effects towards

ibuprofen storage and release.

Amount of AP-TESAmount of AP-TES

Samples% func.

(TGA/DTA)

MCM-41 Irregular Fun. 13%

MCM-41 spher 490 nm + Fun 12%



Samples %C %H %N

MCM-41 Irregular Fun 9,91 2,75 3,26

MCM-41 spher 490 nm + Fun 8,46 2,38 2,76

MCM-41 spher 615 nm + Fun 9,52 2,74 3,04

MCM-41 spher 770 nm+ Fun 9,28 2,61 2,97


SamplesDp

(nm) Vp

(cm3/g)SBET

(m2/g)

MCM-41 IRR 3,4 0,80 928

MCM-41 IRR + fun. 2,69 0,23 341

MCM-41 IRR + fun + ibu - 0,05 30

MCM-41 IRR + fun after ibu rel - 0,24 122

Samples characterizationSamples characterization


After the functionalization the release profile is slower for all the samples After 9 hours the 50% of drug was released It can be clearly seen that spherical particles release more slowly than irregular particles



IBUPROFEN UPTAKE

• The ibuprofen uptake is the same in all samples with magnetic stirring.

• It can be seen the influence of particles morphology in the uptake with orbital stirring.

• The amount of ibuprofen uptake is slower with orbital stirring than magnetic stirring, in the same conditions.

ConclusionsConclusions

• Spherical particles release the drug more slowly then irregular particles.

• Smaller are the spherical particles, slower is the ibuprofen release.

• After the functionalization the release profile is slower for all the samples.

IBUPROFEN RELEASE


thank you for your

attention!

Research funded by MIUR (Project COFIN2006, Prot. 2006032335, Area 03 ), Consortium INSTM and Center of Excellence for Nanostructured Interfaces and Surfaces (University of Torino, Italy).

AcknowledgementsAcknowledgements

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INFLUENCE OF MCM-41 PARTICLES MORPHOLOGY AND FUNCTIONALIZATION ON IBUPROFEN UPTAKE AND RELEASE VI Convegno Nazionale sulla Scienza e Tecnologia dei Materiali