Chitosan as an ocular drug delivery vehicle for vancomycin

Abstract

ABSTRACT:The main objective of this research has been to study the efficiency of chitosan as an ocular drug delivery vehicle for topically applied vancomycin in rabbit eyes. Vancomycin 50 mg/mL was reconstituted in four preparations, namely: in Tears Naturale II TM , in 0.9% w/v aqueous sodium chloride, and in 0.1% and 0.3% w/v chitosan solutions in 1% aqueous L(þ)-lactic acid. Twenty-five microliters of vancomycin (50 mg/mL) were applied into the lower conjunctival eye sac in rabbit eyes. Tear samples were then collected after 0, 30, 60, 90, and 120 min to evaluate the pharmacokinetics of the topically applied vancomycin. Comparison of the results obtained showed that vancomycin 50 mg/mL eye drops in the 0.3% chitosan solution were similar to Tears Naturale II TM in terms of bioavailability. The main conclusion to be drawn from this study is that the 0.3% w/v chitosan solution appears to be a highly promising, cost effective candidate for biomedical use as a vehicle for vancomycin ocular drug delivery.

Comparison of Vehicles for Vancomycin Drug Delivery in Extemporaneously Prepared Ophthalmic Solutions

“…Vancomycin 50 mg/ml in extemporaneous eye drops has been reported in vehicles such as artificial tear and sterile water for injection [3,8]. Chitosan of moisture content, degree of deacetylation (DD) and viscosity-average molecular weight ( v Μ ) of 13.09%, 94.0% and 6.03x10 5 has also been used [9]. The kinematic viscosities of 0.3% w/v chitosan, 0.3%, 0.4% w/v HPMC pH 7.1, Tears Naturale II TM and 0.9% sodium chloride solution were 4.17, 5.24, 9.21, 6.00 and 0.88 mm 2 /s respectively.…”

“…Khangtragool et al [4] found that vancomycin 50 mg/ml in Tears Naturale II TM and 0.9% sodium chloride solution are slightly more acidic than the accepted range (pH 3.5-10.5). Hydroxypropyl methylcellulose (HPMC, Methocel E4M) is preferred in formulations for ophthalmic use [5].…”

Drug delivery system based on poly(ether‐block‐amide) and acrylic acid for controlled release of vancomycin

“…17,18 In this sense, grafting polymerization initiated by the action of gamma radiation is a useful technique for the surface functionalization. 21 PAAc is particularly suitable for biomedical applications since the carboxylic acid groups can be further conjugated with bioactive substances such as drugs, peptides, or antibodies. Also, this technique does not require the use of initiators or additives which may be damaging and difficult to remove.…”

“…20 Thus, the aim of this work was to graft by means of gamma radiation, poly(acrylic acid) (PAAc) onto PEBA films in order to endow them with ability to load vancomycin, a broadspectrum antimicrobial agent. 21 PAAc is particularly suitable for biomedical applications since the carboxylic acid groups can be further conjugated with bioactive substances such as drugs, peptides, or antibodies. 22,23 As far as we know, there are no reports about the modification of PEBA copolymers with hydrophilic polymers as PAAc using gamma radiation neither on loading nor on release of antimicrobial agents for PEBA copolymers.…”