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Microfibrillar polymeric ocular inserts for triamcinolone acetonide delivery.
Int J Pharm. 2019 Aug 15; 567:118459.IJ

Abstract

Despite eye drops generally represent the most convenient, simple and patient-friendly formulations to treat ocular diseases, they suffer from poor retention on the ocular surface and low drug bioavailability leading to the necessity of prolonged and continuous treatment over time. Therefore, ocular insert could represent an innovative way to benefit from ocular topical administration while minimizing all the relevant limitation related to this route of administration. Polymeric non-erodible mucoadhesive ocular inserts should be comfortable and should rapidly adhere on the ocular surface, remain in situ for prolonged period, assure a reproducible and controlled drug release as well as act as transcorneal absorption promoters. In this study, a well-known aliphatic polyester, poly(1,4-butylene succinate) (PBS), was used as starting material to produce hydrophobic microfibrillar scaffolds by means of electrospinning technique. Plasma-assisted chemical surface functionalization of the PBS scaffolds with appropriate biopolymers (inulin, α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide, heparin) was carried out to confer to the final ocular inserts ad hoc properties as wettability, mucoadhesion and cytocompatibility on human corneal epithelial cells, by improving surface hydrophilicity without modifying the bulk properties of the material. The lipophilic drug triamcinolone acetonide was loaded into the obtained ocular insert and release studies were carried out to demonstrate the ability of drug loaded inserts to release the active until 30 days.

Authors+Show Affiliations

Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy(1); Istituto di Biofisica, Consiglio Nazionale delle Ricerche, Via Ugo La Malfa 153, 90146 Palermo, Italy.Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy(1). Electronic address: mariano.licciardi@unipa.it.Advanced Technologies Network Center (ATeN Center), University of Palermo, Viale Delle Scienze - Edificio 18, 90128 Palermo, Italy.Dipartimento di Discipline Chirurgiche, Oncologiche e Stomatologiche (DICHIRONS), Università degli Studi di Palermo, Via Liborio Giuffrè 5, 90127 Palermo, Italy.Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy(1).Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy(1).

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31247275

Citation

Di Prima, Giulia, et al. "Microfibrillar Polymeric Ocular Inserts for Triamcinolone Acetonide Delivery." International Journal of Pharmaceutics, vol. 567, 2019, p. 118459.
Di Prima G, Licciardi M, Carfì Pavia F, et al. Microfibrillar polymeric ocular inserts for triamcinolone acetonide delivery. Int J Pharm. 2019;567:118459.
Di Prima, G., Licciardi, M., Carfì Pavia, F., Lo Monte, A. I., Cavallaro, G., & Giammona, G. (2019). Microfibrillar polymeric ocular inserts for triamcinolone acetonide delivery. International Journal of Pharmaceutics, 567, 118459. https://doi.org/10.1016/j.ijpharm.2019.118459
Di Prima G, et al. Microfibrillar Polymeric Ocular Inserts for Triamcinolone Acetonide Delivery. Int J Pharm. 2019 Aug 15;567:118459. PubMed PMID: 31247275.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Microfibrillar polymeric ocular inserts for triamcinolone acetonide delivery. AU - Di Prima,Giulia, AU - Licciardi,Mariano, AU - Carfì Pavia,Francesco, AU - Lo Monte,Attilio Ignazio, AU - Cavallaro,Gennara, AU - Giammona,Gaetano, Y1 - 2019/06/24/ PY - 2019/04/23/received PY - 2019/06/19/revised PY - 2019/06/23/accepted PY - 2019/6/28/pubmed PY - 2019/12/31/medline PY - 2019/6/28/entrez KW - Electrospinning KW - Ocular insert KW - Plasma-assisted surface functionalization KW - Poly(butylene succinate) (PBS) KW - Triamcinolone acetonide SP - 118459 EP - 118459 JF - International journal of pharmaceutics JO - Int J Pharm VL - 567 N2 - Despite eye drops generally represent the most convenient, simple and patient-friendly formulations to treat ocular diseases, they suffer from poor retention on the ocular surface and low drug bioavailability leading to the necessity of prolonged and continuous treatment over time. Therefore, ocular insert could represent an innovative way to benefit from ocular topical administration while minimizing all the relevant limitation related to this route of administration. Polymeric non-erodible mucoadhesive ocular inserts should be comfortable and should rapidly adhere on the ocular surface, remain in situ for prolonged period, assure a reproducible and controlled drug release as well as act as transcorneal absorption promoters. In this study, a well-known aliphatic polyester, poly(1,4-butylene succinate) (PBS), was used as starting material to produce hydrophobic microfibrillar scaffolds by means of electrospinning technique. Plasma-assisted chemical surface functionalization of the PBS scaffolds with appropriate biopolymers (inulin, α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide, heparin) was carried out to confer to the final ocular inserts ad hoc properties as wettability, mucoadhesion and cytocompatibility on human corneal epithelial cells, by improving surface hydrophilicity without modifying the bulk properties of the material. The lipophilic drug triamcinolone acetonide was loaded into the obtained ocular insert and release studies were carried out to demonstrate the ability of drug loaded inserts to release the active until 30 days. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/31247275/Microfibrillar_polymeric_ocular_inserts_for_triamcinolone_acetonide_delivery_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(19)30493-4 DB - PRIME DP - Unbound Medicine ER -