Publication: Desarrollo y caracterización de nanosistemas farmacéuticos de administración ocular para aumentar la biodisponibilidad de sustancias activas poco hidrosolubles
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2018-11-06
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Universidad Complutense de Madrid
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Abstract
La biodisponibilidad de los fármacos administrados por vía tópica viene condicionada tanto por las especiales características anatomofisiológicas del ojo, como por la naturaleza del principio activo y de la forma dosificación utilizada para su administración. En este último aspecto es en el que se centra esta memoria. Los sistemas nanoparticulares han sido ampliamente estudiados como sistemas de liberación de fármacos en el campo farmacéutico y médico. A nivel ocular, estos sistemas, han demostrado una capacidad de liberar fármacos en localizaciones diana y proporcionar alternativas a diferentes tratamientos convencionales. El glaucoma es una de las enfermedades oculares más importantes por ser la principal causa de ceguera en los países industrializados. Esta patología está caracterizada por una pérdida de las células ganglionares de la retina (RGCs) y sus axones. En esta enfermedad, es frecuente el incremento de la presión intraocular (PIO > 21 mmHg), produciendo un daño irreversible en el nervio óptico, seguido de una neuropatía ocular y perdida de la visión. Por esta razón, los agentes hipotensores oculares se han convertido en los componentes principales en el tratamiento de la enfermedad. La acetazolamida (ACZ) es una sustancia activa inhibidora de la anhidrasa carbónica estando aprobada su utilización por vía oral como reductor de la presión intraocular en el tratamiento del glaucoma. Sin embargo, su prescripción está bastante limitada debido a los potenciales efectos adversos sistémicos que puede generar. Además, su hidrosolubilidad es muy baja (0,7 mg/mL) y su permeabilidad corneal está muy limitada. Estas condiciones suponen nuevos retos en el desarrollo de formulaciones de aplicación tópica ocular...
The bioavailability of topically administered drugs is conditioned by the special anatomo-physiological characteristics of the eye, the nature of the active substance and the dosage form used for its administration. In this last aspect is where this memory is focused. Nanoparticular systems have been widely studied as drug delivery systems in the pharmaceutical and medical fields. At ocular level, these systems have demonstrated an ability to release drugs at target sites and provide alternatives to different conventional treatments. Glaucoma is one of the most important eye diseases since it is the leading cause of blindness in industrialized countries. This pathology is characterized by a loss of retinal ganglion cells (RGCs) and their axons. In this disease, an increase in intraocular pressure (IOP > 21 mmHg) is common, leading to irreversible damage to the optic nerve, followed by ocular neuropathy and loss of vision. For this reason, ocular hypotensive agents have become the main drug agents used in the treatment of the disease. Acetazolamide (ACZ) is an active substance that inhibits carbonic anhydrase and its use as an oral intraocular pressure reducer is approved for the treatment of glaucoma. However, its prescription is quite limited due to the potential systemic adverse effects that can generate with the use of this route of administration. In addition, its water solubility is very low (0.7 mg/mL) and its corneal permeability is very limited. For all of the above, the development of topical ocular acetazolamide formulations is a technological challenge...
The bioavailability of topically administered drugs is conditioned by the special anatomo-physiological characteristics of the eye, the nature of the active substance and the dosage form used for its administration. In this last aspect is where this memory is focused. Nanoparticular systems have been widely studied as drug delivery systems in the pharmaceutical and medical fields. At ocular level, these systems have demonstrated an ability to release drugs at target sites and provide alternatives to different conventional treatments. Glaucoma is one of the most important eye diseases since it is the leading cause of blindness in industrialized countries. This pathology is characterized by a loss of retinal ganglion cells (RGCs) and their axons. In this disease, an increase in intraocular pressure (IOP > 21 mmHg) is common, leading to irreversible damage to the optic nerve, followed by ocular neuropathy and loss of vision. For this reason, ocular hypotensive agents have become the main drug agents used in the treatment of the disease. Acetazolamide (ACZ) is an active substance that inhibits carbonic anhydrase and its use as an oral intraocular pressure reducer is approved for the treatment of glaucoma. However, its prescription is quite limited due to the potential systemic adverse effects that can generate with the use of this route of administration. In addition, its water solubility is very low (0.7 mg/mL) and its corneal permeability is very limited. For all of the above, the development of topical ocular acetazolamide formulations is a technological challenge...
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Tesis de la Universidad Complutense de Madrid, Facultad de Farmacia, Departamento de Farmacia y Tecnología Farmacéutica, leída el 12/09/2017