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Nonpolymeric nanoassemblies for ocular administration of acyclovir: pharmacokinetic evaluation in rabbits.
Eur J Pharm Biopharm. 2012 Jan; 80(1):39-45.EJ

Abstract

The aim of this study was to increase bioavailability of the antiviral drug acyclovir (ACV) when administered by the ocular route. For this purpose, a new lipophilic derivative of acyclovir was synthesized, both possessing greater lipophilicity and providing the formation of a homogeneous water dispersion with higher amount of ACV than the aqueous solution of the parent drug. This was done by chemically linking acyclovir to the isoprenoid chain of squalene, obtaining 4'-trisnorsqualenoylacyclovir (SQACV), in which squalene is covalently coupled to the 4'-hydroxy group of acyclovir. This new prodrug was then formulated as nonpolymeric nanoassemblies through nanoprecipitation; the resulting particles were characterized in terms of mean diameter, zeta potential, and stability. The pharmacokinetic profile of the prodrug in the tear fluid and in the aqueous humor of rabbits was evaluated and compared to that of the parent drug. Data showed that SQACV nanoassemblies increased the amount of ACV in the aqueous humor of rabbits compared to free ACV solution. This new amphiphilic prodrug of acyclovir is a very promising tool to increase the ocular bioavailability of the parent drug.

Authors+Show Affiliations

Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Torino, Italy.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22008147

Citation

Stella, Barbara, et al. "Nonpolymeric Nanoassemblies for Ocular Administration of Acyclovir: Pharmacokinetic Evaluation in Rabbits." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 80, no. 1, 2012, pp. 39-45.
Stella B, Arpicco S, Rocco F, et al. Nonpolymeric nanoassemblies for ocular administration of acyclovir: pharmacokinetic evaluation in rabbits. Eur J Pharm Biopharm. 2012;80(1):39-45.
Stella, B., Arpicco, S., Rocco, F., Burgalassi, S., Nicosia, N., Tampucci, S., Chetoni, P., & Cattel, L. (2012). Nonpolymeric nanoassemblies for ocular administration of acyclovir: pharmacokinetic evaluation in rabbits. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 80(1), 39-45. https://doi.org/10.1016/j.ejpb.2011.10.001
Stella B, et al. Nonpolymeric Nanoassemblies for Ocular Administration of Acyclovir: Pharmacokinetic Evaluation in Rabbits. Eur J Pharm Biopharm. 2012;80(1):39-45. PubMed PMID: 22008147.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Nonpolymeric nanoassemblies for ocular administration of acyclovir: pharmacokinetic evaluation in rabbits. AU - Stella,Barbara, AU - Arpicco,Silvia, AU - Rocco,Flavio, AU - Burgalassi,Susi, AU - Nicosia,Nadia, AU - Tampucci,Silvia, AU - Chetoni,Patrizia, AU - Cattel,Luigi, Y1 - 2011/10/08/ PY - 2011/05/09/received PY - 2011/09/30/revised PY - 2011/10/03/accepted PY - 2011/10/20/entrez PY - 2011/10/20/pubmed PY - 2012/7/3/medline SP - 39 EP - 45 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 80 IS - 1 N2 - The aim of this study was to increase bioavailability of the antiviral drug acyclovir (ACV) when administered by the ocular route. For this purpose, a new lipophilic derivative of acyclovir was synthesized, both possessing greater lipophilicity and providing the formation of a homogeneous water dispersion with higher amount of ACV than the aqueous solution of the parent drug. This was done by chemically linking acyclovir to the isoprenoid chain of squalene, obtaining 4'-trisnorsqualenoylacyclovir (SQACV), in which squalene is covalently coupled to the 4'-hydroxy group of acyclovir. This new prodrug was then formulated as nonpolymeric nanoassemblies through nanoprecipitation; the resulting particles were characterized in terms of mean diameter, zeta potential, and stability. The pharmacokinetic profile of the prodrug in the tear fluid and in the aqueous humor of rabbits was evaluated and compared to that of the parent drug. Data showed that SQACV nanoassemblies increased the amount of ACV in the aqueous humor of rabbits compared to free ACV solution. This new amphiphilic prodrug of acyclovir is a very promising tool to increase the ocular bioavailability of the parent drug. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/22008147/Nonpolymeric_nanoassemblies_for_ocular_administration_of_acyclovir:_pharmacokinetic_evaluation_in_rabbits_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(11)00296-7 DB - PRIME DP - Unbound Medicine ER -