Development of prednisolone-containing eye drop formulations by cyclodextrin complexation and antimicrobial, mucoadhesive biopolymer

Tivadar Bíró, Gabriella Horvát, Mária Budai-Szűcs, Erzsébet Csányi, E. Urbán, Andrea Facskó, P. Szabó-Révész, Ildikó Csóka, Z. Aigner

Research output: Article

1 Citation (Scopus)

Abstract

Purpose: The formulation of topical ophthalmic products with appropriate therapeutic effect and patient compliance is a major challenge. To increase the efficiency of the ocular delivery of the drug, the enhancement of water solubility and the contact time of the drug on the surface of the cornea are necessary. In this work, prednisolone (PR)-containing eye drops were formulated with antimicrobial, mucoadhesive biopolymer and PR–cyclodextrin inclusion complex. This approach can be used for the development of innovative ophthalmic formulations. Materials and methods: After adjusting the optimal physiological parameters, the amount of the required cyclodextrin for the highest penetration of PR was determined by dialysis membrane diffusion study. The viscosity, surface tension and mucoadhesion of the eye drops were measured. The microbiological effectiveness of zinc-hyaluronate (ZnHA) was investigated by a standard method of the European Pharmacopoeia. Results: In this case, no significant difference of surface tension was measured in products with different amounts of cyclodextrin. According to the results of the tensile test, ZnHA as a mucoadhesive biopolymer improves the mucoadhesion of ophthalmic products. The antimicrobial stability of formulations preserved by ZnHA meets requirement B of the European Pharmacopoeia. Conclusion: It can be stated that the innovative PR-containing compositions are suitable for producing mucoadhesive, properly preserved aqueous ophthalmic solutions with increased bioavailability attributes.

Original languageEnglish
Pages (from-to)2529-2537
Number of pages9
JournalDrug Design, Development and Therapy
Volume12
DOIs
Publication statusPublished - jan. 1 2018

Fingerprint

Biopolymers
Ophthalmic Solutions
Cyclodextrins
Prednisolone
Pharmacopoeias
Surface Tension
Therapeutic Uses
Patient Compliance
Viscosity
Pharmaceutical Preparations
Solubility
Cornea
Biological Availability
Dialysis
Membranes
Water
zinc hyaluronate complex

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery

Cite this

Development of prednisolone-containing eye drop formulations by cyclodextrin complexation and antimicrobial, mucoadhesive biopolymer. / Bíró, Tivadar; Horvát, Gabriella; Budai-Szűcs, Mária; Csányi, Erzsébet; Urbán, E.; Facskó, Andrea; Szabó-Révész, P.; Csóka, Ildikó; Aigner, Z.

In: Drug Design, Development and Therapy, Vol. 12, 01.01.2018, p. 2529-2537.

Research output: Article

Bíró, Tivadar ; Horvát, Gabriella ; Budai-Szűcs, Mária ; Csányi, Erzsébet ; Urbán, E. ; Facskó, Andrea ; Szabó-Révész, P. ; Csóka, Ildikó ; Aigner, Z. / Development of prednisolone-containing eye drop formulations by cyclodextrin complexation and antimicrobial, mucoadhesive biopolymer. In: Drug Design, Development and Therapy. 2018 ; Vol. 12. pp. 2529-2537.
@article{731215402adb4701b9d68fe0cf4bece8,
title = "Development of prednisolone-containing eye drop formulations by cyclodextrin complexation and antimicrobial, mucoadhesive biopolymer",
abstract = "Purpose: The formulation of topical ophthalmic products with appropriate therapeutic effect and patient compliance is a major challenge. To increase the efficiency of the ocular delivery of the drug, the enhancement of water solubility and the contact time of the drug on the surface of the cornea are necessary. In this work, prednisolone (PR)-containing eye drops were formulated with antimicrobial, mucoadhesive biopolymer and PR–cyclodextrin inclusion complex. This approach can be used for the development of innovative ophthalmic formulations. Materials and methods: After adjusting the optimal physiological parameters, the amount of the required cyclodextrin for the highest penetration of PR was determined by dialysis membrane diffusion study. The viscosity, surface tension and mucoadhesion of the eye drops were measured. The microbiological effectiveness of zinc-hyaluronate (ZnHA) was investigated by a standard method of the European Pharmacopoeia. Results: In this case, no significant difference of surface tension was measured in products with different amounts of cyclodextrin. According to the results of the tensile test, ZnHA as a mucoadhesive biopolymer improves the mucoadhesion of ophthalmic products. The antimicrobial stability of formulations preserved by ZnHA meets requirement B of the European Pharmacopoeia. Conclusion: It can be stated that the innovative PR-containing compositions are suitable for producing mucoadhesive, properly preserved aqueous ophthalmic solutions with increased bioavailability attributes.",
keywords = "Membrane diffusion, Microbiological stability, Ocular drug delivery, Pharmaceutical formulation, Zinc-hyaluronate",
author = "Tivadar B{\'i}r{\'o} and Gabriella Horv{\'a}t and M{\'a}ria Budai-Szűcs and Erzs{\'e}bet Cs{\'a}nyi and E. Urb{\'a}n and Andrea Facsk{\'o} and P. Szab{\'o}-R{\'e}v{\'e}sz and Ildik{\'o} Cs{\'o}ka and Z. Aigner",
year = "2018",
month = "1",
day = "1",
doi = "10.2147/DDDT.S165693",
language = "English",
volume = "12",
pages = "2529--2537",
journal = "Drug Design, Development and Therapy",
issn = "1177-8881",
publisher = "Dove Medical Press Ltd.",

}

TY - JOUR

T1 - Development of prednisolone-containing eye drop formulations by cyclodextrin complexation and antimicrobial, mucoadhesive biopolymer

AU - Bíró, Tivadar

AU - Horvát, Gabriella

AU - Budai-Szűcs, Mária

AU - Csányi, Erzsébet

AU - Urbán, E.

AU - Facskó, Andrea

AU - Szabó-Révész, P.

AU - Csóka, Ildikó

AU - Aigner, Z.

PY - 2018/1/1

Y1 - 2018/1/1

N2 - Purpose: The formulation of topical ophthalmic products with appropriate therapeutic effect and patient compliance is a major challenge. To increase the efficiency of the ocular delivery of the drug, the enhancement of water solubility and the contact time of the drug on the surface of the cornea are necessary. In this work, prednisolone (PR)-containing eye drops were formulated with antimicrobial, mucoadhesive biopolymer and PR–cyclodextrin inclusion complex. This approach can be used for the development of innovative ophthalmic formulations. Materials and methods: After adjusting the optimal physiological parameters, the amount of the required cyclodextrin for the highest penetration of PR was determined by dialysis membrane diffusion study. The viscosity, surface tension and mucoadhesion of the eye drops were measured. The microbiological effectiveness of zinc-hyaluronate (ZnHA) was investigated by a standard method of the European Pharmacopoeia. Results: In this case, no significant difference of surface tension was measured in products with different amounts of cyclodextrin. According to the results of the tensile test, ZnHA as a mucoadhesive biopolymer improves the mucoadhesion of ophthalmic products. The antimicrobial stability of formulations preserved by ZnHA meets requirement B of the European Pharmacopoeia. Conclusion: It can be stated that the innovative PR-containing compositions are suitable for producing mucoadhesive, properly preserved aqueous ophthalmic solutions with increased bioavailability attributes.

AB - Purpose: The formulation of topical ophthalmic products with appropriate therapeutic effect and patient compliance is a major challenge. To increase the efficiency of the ocular delivery of the drug, the enhancement of water solubility and the contact time of the drug on the surface of the cornea are necessary. In this work, prednisolone (PR)-containing eye drops were formulated with antimicrobial, mucoadhesive biopolymer and PR–cyclodextrin inclusion complex. This approach can be used for the development of innovative ophthalmic formulations. Materials and methods: After adjusting the optimal physiological parameters, the amount of the required cyclodextrin for the highest penetration of PR was determined by dialysis membrane diffusion study. The viscosity, surface tension and mucoadhesion of the eye drops were measured. The microbiological effectiveness of zinc-hyaluronate (ZnHA) was investigated by a standard method of the European Pharmacopoeia. Results: In this case, no significant difference of surface tension was measured in products with different amounts of cyclodextrin. According to the results of the tensile test, ZnHA as a mucoadhesive biopolymer improves the mucoadhesion of ophthalmic products. The antimicrobial stability of formulations preserved by ZnHA meets requirement B of the European Pharmacopoeia. Conclusion: It can be stated that the innovative PR-containing compositions are suitable for producing mucoadhesive, properly preserved aqueous ophthalmic solutions with increased bioavailability attributes.

KW - Membrane diffusion

KW - Microbiological stability

KW - Ocular drug delivery

KW - Pharmaceutical formulation

KW - Zinc-hyaluronate

UR - http://www.scopus.com/inward/record.url?scp=85057828419&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85057828419&partnerID=8YFLogxK

U2 - 10.2147/DDDT.S165693

DO - 10.2147/DDDT.S165693

M3 - Article

VL - 12

SP - 2529

EP - 2537

JO - Drug Design, Development and Therapy

JF - Drug Design, Development and Therapy

SN - 1177-8881

ER -