Dexamethasone-loaded poly(ε-caprolactone) intravitreal implants: A pilot study

Fialho, Sílvia Ligório; Behar‐Cohen, Francine; Silva-Cunha, Armando

doi:10.1016/j.ejpb.2007.08.004

Cited by 75 publications

(42 citation statements)

References 33 publications

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“…O perfil de liberação obtido no presente estudo é parecido com outros perfis de sistemas poliméricos relatados em diferentes trabalhos (5,16,20) . Em geral, o perfil de liberação pode ser dividido em três etapas: a primeira consiste de uma alta taxa de liberação do fármaco, conhecida como "burst" inicial, possivelmente devido à presença do fármaco na superfície do sistema (20) .…”

Section: Discussionunclassified

“…A utilização da poli-ε-caprolactona (PCL) na preparação de SLF tem sido bastante explorada nos últimos anos. Estudos de eficácia e biocompatibilidade da PCL resultaram na sua aprovação pela "Food and Drug Administration" para utilização farmacêutica (5) . A prednisolona, assim como os outros corticóides, diminui ou impede a resposta tissular ao processo inflamatório, por intermédio da redução do desenvolvimento dos sintomas da inflamação (6) .…”

Section: Resumo Introduçãounclassified

See 1 more Smart Citation

Sistemas biodegradáveis contendo acetato de prednisolona para administração orbitária

Byrro¹,

Miyashita²,

Albuquerque³

et al. 2009

Arq. Bras. Oftalmol.

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Section: Discussionunclassified

Section: Resumo Introduçãounclassified

Sistemas biodegradáveis contendo acetato de prednisolona para administração orbitária

Byrro¹,

Miyashita²,

Albuquerque³

et al. 2009

Arq. Bras. Oftalmol.

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“…Fialho et al also developed poly-e-caprolactone (PCL) implants containing dexamethasone (Fialho et al, 2008;Fialho et al, 2009). These implants released dexamethasone concentrations in vitro, indicating their potential for suppressing several inflammatory processes.…”

Section: Biodegradable Implants In the Treatment Of Uveitismentioning

confidence: 99%

“…However, the degradation rate of PCL is slow (2 to 3 years) (Bourges et al, 2006;Nair, Laurencin, 2007). The slow degradation, high biocompatibility, and high permeability of drugs are characteristics of PCL that have been investigated to develop controlled drug delivery devices in the eye (Kimura, Ogura, 2001;Dong et al, 2006;Peyman, Ganiban, 2006;Fialho et al, 2008).…”

Section: Biodegradable Implantsmentioning

confidence: 99%

Implants as drug delivery devices for the treatment of eye diseases

Silva

Fialho

Siqueira³

et al. 2010

Braz. J. Pharm. Sci.

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The treatment of diseases affecting the posterior segment of the eye is limited by the difficulty in transporting effective doses of drugs to the vitreous, retina, and choroid. Topically applied drugs are poorly absorbed due to the low permeability of the external ocular tissues and tearing. The blood-retina barrier limits drug diffusion from the systemic blood to the posterior segment, thus high doses of drug are needed to maintain therapeutic levels. In addition, systemic side effects are common. Intraocular injections could be an alternative, but the fast flowing blood supply in this region, associated with rapid clearance rates, causes drug concentration to quickly fall below therapeutic levels. To obtain therapeutic levels over longer time periods, polymeric sustained-drug release systems implanted within the vitreous are being studied for the treatment of vitreoretinal disorders. These systems are prepared using different kinds of biodegradable or non-biodegradable polymers. This review aims to demonstrate the main characteristics of these drug delivery implants and their potential for clinical application.Uniterms: Implants/biodegradation. Drugs/delivery systems. Drugs/prolonged delivery systems. Pharmaceutical technology.O tratamento de doenças do segmento posterior do olho é limitado pela dificuldade no transporte de doses efetivas de fármacos para o vítreo, retina e coróide. Os fármacos aplicados topicamente são pouco absorvidos por causa da baixa permeabilidade dos tecidos oculares externos e ao lacrimejamento. Embora a administração sistêmica seja capaz de transportar fármacos para o segmento posterior do olho, as barreiras hemato-aquosa e hematorretiniana dificultam a absorção e, normalmente, são necessárias doses elevadas, as quais estão geralmente associadas a potenciais efeitos adversos. Injeções intravitreais são capazes de transportar fármacos para o segmento posterior do olho, mas é uma técnica invasiva, pouco tolerada pelos pacientes e apresenta riscos de infecções oculares e danos aos tecidos. Visando a obtenção de níveis terapêuticos adequados de fármacos no segmento posterior do bulbo do olho por longos períodos, sistemas de liberação poliméricos implantados diretamente no vítreo estão sendo investigados para o tratamento de várias doenças vítreo-retinianas. Esses implantes podem ser preparados a partir de diferentes polímeros biocompatíveis, biodegradáveis ou não-biodegradáveis. Nesta revisão, as principais características destes implantes transportadores de fármacos são descritas, expondo suas potencialidades de aplicação clínica.Unitermos: Implantes oculares/biodegradação. Fármacos/sistemas de liberação. Fármacos/ Fármacos/ ação prolongada. Tecnologia farmacêutica.

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“…Hot-melt extrusion (HME) is a thermal processing technique that has received considerable attention as a new approach for the development of polymeric sustained release systems (Jain, 2000;Fialho et al, 2008;Ghalanbor et al, 2010;Roblegg et al, 2011;Zema et al, 2012). The process is continuous, simple and efficient.…”

Section: Introductionmentioning

confidence: 99%

PLA/PEG-PPG-PEG/Dexamethasone implant prepared by hot-melt extrusion for controlled release of immunosuppressive drug to implantable medical devices, part 2:in vivoevaluation

Li¹,

Guo²,

Deng³

et al. 2013

Drug Delivery

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Hot-melt extrusion (HME) plays an important role in preparing implants as local drug delivery systems in pharmaceutical fields. Here, a new PLA/PEG-PPG-PEG/Dexamethasone (PLA/F68/ Dex) implant prepared by HME has been developed. Importantly, the implant was successfully achieved to control release of immunosuppressive drug to an implanted device. In particular, this implant has not been reported previously in pharmaceutical fields. FTIR and XRD were adopted to investigate the properties of the samples. The in vivo release study showed that the maximum value of Dex release from the implants was approximately 50% at 1 month. The in vivo degradation behavior was determined by UV spectrophotometer and scanning electron microscopy studies, and the weight loss rate of the implants were up to 25% at 1 month. Furthermore, complete blood count (CBC) test, serum chemistry and major organs were performed, and there is no significant lesion and side effects observed in these results. Therefore, the results elucidated that the new PLA/F68/Dex implant prepared by HME could deliver an immunosuppressive drug to control the inflammatory reaction at the implant site.

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Dexamethasone-loaded poly(ε-caprolactone) intravitreal implants: A pilot study

Cited by 75 publications

References 33 publications

Sistemas biodegradáveis contendo acetato de prednisolona para administração orbitária

Sistemas biodegradáveis contendo acetato de prednisolona para administração orbitária

Implants as drug delivery devices for the treatment of eye diseases

PLA/PEG-PPG-PEG/Dexamethasone implant prepared by hot-melt extrusion for controlled release of immunosuppressive drug to implantable medical devices, part 2:in vivoevaluation

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