Gellan-based systems for ophthalmic sustained delivery of methylprednisolone

Sanzgiri, Yeshwant D.; Maschi, Sergio; Crescenzi, V.; Callegaro, L.; Topp, Elizabeth M.; Stella, Valentino J.

doi:10.1016/0168-3659(93)90186-9

Cited by 102 publications

(34 citation statements)

References 14 publications

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“…In the past few years, an impressive number of pH (e.g., cellulose acetate phthalate and Carbopol), temperature (e.g., Poloxamer), and ion (e.g., gellan gum and alginate) induced in situ forming systems have been reported to sustain ophthalmic drug delivery (8)(9)(10)(11). These in situ gel-forming systems could prolong the precorneal residence time of a drug (12)(13)(14)(15)(16) and improve ocular bioavailability (17). The choice of a special hydrogel depends on its intrinsic properties and envisaged therapeutic use.…”

Section: Introductionmentioning

confidence: 99%

In Situ Gelling Gelrite/Alginate Formulations as Vehicles for Ophthalmic Drug Delivery

Liu

Zhang

et al. 2010

AAPS PharmSciTech

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Abstract. The objective of this study was to develop an ion-activated in situ gelling vehicle for ophthalmic delivery of matrine. The rheological properties of polymer solutions, including Gelrite, alginate, and Gelrite/alginate solution, were evaluated. In addition, the effect of formulation characteristics on in vitro release and in vivo precorneal drug kinetic of matrine was investigated. It was found that the optimum concentration of Gelrite solution for the in situ gel-forming delivery systems was 0.3% (w/w) and that for alginate solution was 1.4% (w/w). The mixture of 0.2% Gelrite and 0.6% alginate solutions showed a significant enhancement in gel strength at physiological condition. On the basis of the in vitro results, the Gelrite formulations of matrine-containing alginate released the drug most slowly. For each tested polymer solution, the concentration of matrine in the precorneal area was higher than that of matrinecontaining simulated tear fluid (STF) almost at each time point (p<0.05). The area under the curve of formulation 16 (0.2%Gelrite/0.6%alginate) was 4.65 times greater than that of containing matrine STF. Both the in vitro release and in vivo pharmacological studies indicated that the Gelrite/alginate solution had the better ability to retain drug than the Gelrite or alginate solutions alone. The tested formulation was found to be almost non-irritant in the ocular irritancy test. The overall results of this study revealed that the Gelrite/alginate mixture can be used as an in situ gelling vehicle to enhance ocular retention.

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Section: Introductionmentioning

confidence: 99%

In Situ Gelling Gelrite/Alginate Formulations as Vehicles for Ophthalmic Drug Delivery

Liu

Zhang

et al. 2010

AAPS PharmSciTech

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“…[12][13][14] It is commonly applied in the food industry, 15 and has been previously used in the biomedical field for drug delivery. 16 Gellan gum has been originally proposed by our group 17 as a new biomaterial for cartilage tissue engineering applications, yet recent studies can be found on the same application 18 and on the general use of gellan gum for tissue engineering. 19 In our previous works, it has been used to encapsulate both human nasal and articular chondrocytes in vitro, and has been tested in vivo by subcutaneous implantation in nude mice with human articular chondrocytes.…”

mentioning

confidence: 99%

Injectable gellan gum hydrogels with autologous cells for the treatment of rabbit articular cartilage defects

Oliveira

Gardel

Rada

et al. 2010

Journal Orthopaedic Research

127

104

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In this work, the ability of gellan gum hydrogels coupled with autologous cells to regenerate rabbit full-thickness articular cartilage defects was tested. Five study groups were defined: (a) gellan gum with encapsulated chondrogenic predifferentiated rabbit adipose stem cells (ASC þ GF); (b) gellan gum with encapsulated nonchondrogenic predifferentiated rabbit adipose stem cells (ASC); (c) gellan gum with encapsulated rabbit articular chondrocytes (AC) (standard control); (d) gellan gum alone (control); (e) empty defect (control). Fullthickness articular cartilage defects were created and the gellan gum constructs were injected and left for 8 weeks. The macroscopic aspect of the explants showed a progressive increase of similarity with the lateral native cartilage, stable integration at the defect site, more pronouncedly in the cell-loaded constructs. Tissue scoring showed that ASC þ GF exhibited the best results regarding tissue quality progression. Alcian blue retrieved similar results with a better outcome for the cell-loaded constructs. Regarding real-time PCR analyses, ASC þ GF had the best progression with an upregulation of collagen type II and aggrecan, and a downregulation of collagen type I. Gellan gum hydrogels combined with autologous cells constitute a promising approach for the treatment of articular cartilage defects, and adipose derived cells may constitute a valid alternative to currently used articular chondrocytes. ß

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“…Compared with the MP suspension control, gellan-MP films yielded an approximately 4 fold higher area under tear fluid concentration versus time curve, but exhibited a tendency to slip out of the eye due to a higher degree of swelling. The area under tear fluid concentration of the films was approximately equal to that of the control, while that from the eye drops showed 2.6 fold increases than the control and also provided ease of administration 25 .…”

Section: +mentioning

confidence: 77%

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2012

IJPSR

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Topical administration of a drug in the conjunctival cul-de-sac is the treatment of choice for diseases of the anterior segment of eye. Development of ophthalmic drug delivery systems has always been challenging because of the drawbacks with this route, like non-productive absorption, drainage, induced lacrimation, tear turn over, impermeability of drugs to cornea. New approaches have been investigated for delivery of drugs to the eye by means of polymeric delivery of ophthalmic drugs to the pre-and intra ocular tissues, have been attempted to increase the bioavailability and the duration of therapeutic action of ocular drug. Certain new approaches to increase the ocular bioavailability, duration of the drug action and to reduce the undesirable side effects are by using drug carriers that regulate pre-corneal drug loss and improve the corneal contact time. Many of these systems prolong ocular bioavailability but do not control drug penetration through the cornea. Consequently, the drug concentration at the site of action might remain inadequate. Therefore, it is necessary to develop safer, efficacious and more acceptable ocular therapeutic system. The ocular bioavailability of the drugs can be improved by prolonging their residence time in the cul-de-sac and by increasing their corneal permeability. There are various new dosage forms like in-situ gel, collagen shield, etc.

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Gellan-based systems for ophthalmic sustained delivery of methylprednisolone

Cited by 102 publications

References 14 publications

In Situ Gelling Gelrite/Alginate Formulations as Vehicles for Ophthalmic Drug Delivery

In Situ Gelling Gelrite/Alginate Formulations as Vehicles for Ophthalmic Drug Delivery

Injectable gellan gum hydrogels with autologous cells for the treatment of rabbit articular cartilage defects

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