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Microparticles as Drug Delivery Systems for the Back of the Eye

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Drug Product Development for the Back of the Eye

Part of the book series: AAPS Advances in the Pharmaceutical Sciences Series ((AAPS,volume 2))

Abstract

Treatment of vitreoretinal disorders often include repeated intraocular injections to achieve effective levels of the active substance in the target site. Intraocular drug delivery systems (IDDS) are considered an alternative to multiple injections as they release the encapsulated drug over long periods of time. Among them, biodegradable microparticles are very useful for intraocular administration because they can be injected as a conventional suspension without surgical procedures, to release the active substance over weeks or months. Microparticles can be loaded with different drugs useful to treat different pathologies affecting the back of the eye such as proliferative vitreoretinopathy, age-related macular degeneration, cytomegalovirus retinitis, diabetic retinopathy, endophthalmitis, glaucoma, herpes infection, macular edema, retinal vein occlusion, retinitis pigmentosa, and uveitis. Administration of microparticles can be performed by periocular, intravitreal, subretinal, or other intraocular routes to treat vitreoretinal disorders. Generally, microparticles are loaded with one active substance. Recently, biodegradable microparticles loaded with more than one drug (“combo microparticles”) are being developed. Moreover, biodegradable microspheres are potential tools for retinal repair in combination with retinal progenitor cells.

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Abbreviations

PLA:

Poly(lactic) acid

PGA:

Poly(glycolic) acid

PLGA:

Poly(lactic-co-glycolic) acid

GPC:

Gel permeation chromatography

Mw:

Weight-average molecular weight

Mn:

Number-average molecular weight

PEG:

Polyethylene glycol

kGy:

Kilo Gray

Tg:

Glass transition temperature

Tm:

Crystalline melting points

Css:

Steady state concentration

K0 :

Zero-order constant

Vd :

Volume of the vitreous

\( {K}_{e}\) :

Elimination rate constant

G:

Gauge

PBS:

Phosphate buffer solution

BSS:

Buffer solution

HA:

Hyaluronic acid

HPMC:

Hydroxypropylmethyl cellulose

AUC:

Area under the curve

5-FU:

5-fluorouracil

VEGF:

Vascular Endothelial Growth Factor

AMD:

Age macular degeneration (AMD)

TA:

Triamcinolone acetonide

PVR:

Proliferative vitreoretinopathy

RPE:

Retinal pigment epithelium

RD:

Retinal detachment

RA:

Retinoic acid

LPS:

Lipopolysaccharide

TRD:

Tractional retinal detachment

CyS:

Cyclosporine

CNV:

Choroidal neovascularization

ARN:

Acute retinal necrosis

HSV:

Herpes simplex virus

Da:

Daltons

CMV:

Cytomegalovirus

HCMV:

Human cytomegalovirus

RGC:

Retinal ganglion cells (RGC)

ECM:

Extracellular matrix

MMP2:

Matrix metalloproteinase

RPCs:

Retinal progenitor cells (RPCs)

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Acknowledgments

The author thanks Vanessa Andres and Patricia Checa for their technical assistance. MAT 2010–6528, RETICS RD07/0062, and Research Group 920415 (CG/10) are acknowledged for financial support.

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Authors and Affiliations

  1. Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, Avda Complutense s/n, Complutense University, 28040, Madrid, Spain

    Rocío Herrero-Vanrell PhD

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  1. Rocío Herrero-Vanrell PhD
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Correspondence to Rocío Herrero-Vanrell PhD .

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Editors and Affiliations

  1. School of Pharmacy, University of Colorado Denver, East 17th Avenue 12631, Aurora, 80045, Colorado, USA

    Uday B. Kompella

  2. School of Medicine, Emory University, Clifton Road NE., 1365, Atlanta, 30322, Georgia, USA

    Henry F. Edelhauser

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Herrero-Vanrell, R. (2011). Microparticles as Drug Delivery Systems for the Back of the Eye. In: Kompella, U., Edelhauser, H. (eds) Drug Product Development for the Back of the Eye. AAPS Advances in the Pharmaceutical Sciences Series, vol 2. Springer, Boston, MA. https://doi.org/10.1007/978-1-4419-9920-7_10

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