Limits...
Design and Evaluation of Voriconazole Eye Drops for the Treatment of Fungal Keratitis.

Malhotra S, Khare A, Grover K, Singh I, Pawar P - J Pharm (Cairo) (2014)

Bottom Line: The results revealed that voriconazole drop containing PVA provided least viscosity and higher corneal permeation of drug, while drop formulated with XG had maximum viscosity and least permeation.The microbiological studies showed that voriconazole ophthalmic solution containing xanthan gum shows better antifungal activity as compared to voriconazole and xanthan gum alone.Thus, it can be concluded that HP-β-CD based voriconazole (1.5%, pH 7.0) ophthalmic solution containing BAK and EDTA with viscosity modifier XG provided maximum precorneal residence time as compared to other viscosity modifiers and polyvinyl alcohol provided less precorneal residence time than other viscosity modifiers.

View Article: PubMed Central - PubMed

Affiliation: Chitkara College of Pharmacy, Chitkara University, Chandigarh-Patiala National Highway, Rajpura, Patiala, Punjab, 140401, India.

ABSTRACT
Voriconazole is a novel antifungal agent with excellent broad spectrum activity commercially available for oral and intravenous administration. The purpose of this study was to prepare ophthalmic formulation of hydroxypropyl beta cyclodextrin (HP-β-CD) based voriconazole containing benzalkonium chloride BAK and EDTA with or without viscosity modifiers and study its permeation characteristics through freshly excised goat cornea. The results were observed that viscosity and force of bioadhesion of the voriconazole HP-β-CD solutions containing xanthan gum (XG) are more as compared to polyvinyl alcohol. The results revealed that voriconazole drop containing PVA provided least viscosity and higher corneal permeation of drug, while drop formulated with XG had maximum viscosity and least permeation. The HP-β-CD based voriconazole (1.5%) ophthalmic formulation containing xanthan gum (1.5), preserved with BAK and EDTA, could provide shelf life of 2 years. The microbiological studies showed that voriconazole ophthalmic solution containing xanthan gum shows better antifungal activity as compared to voriconazole and xanthan gum alone. Thus, it can be concluded that HP-β-CD based voriconazole (1.5%, pH 7.0) ophthalmic solution containing BAK and EDTA with viscosity modifier XG provided maximum precorneal residence time as compared to other viscosity modifiers and polyvinyl alcohol provided less precorneal residence time than other viscosity modifiers.

No MeSH data available.


Related in: MedlinePlus

Comparative rheological studies of voriconazole ophthalmic formulations containing different viscosity modifiers. Values are mean ± SE of 3 in each group. PVA refers to polyvinyl alcohol, CS refers to chitosan, GG refers to guar gum, SA refers to sodium alginate, SCMC refers to sodium carboxymethyl cellulose, and XG refers to xanthan gum and gelrite.
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4590801&req=5

fig1: Comparative rheological studies of voriconazole ophthalmic formulations containing different viscosity modifiers. Values are mean ± SE of 3 in each group. PVA refers to polyvinyl alcohol, CS refers to chitosan, GG refers to guar gum, SA refers to sodium alginate, SCMC refers to sodium carboxymethyl cellulose, and XG refers to xanthan gum and gelrite.

Mentions: All the ophthalmic formulations containing different viscosity modifiers show pseudo plastic behavior, that is, high viscosity at low shear rate and low viscosity at high shear rate. The optimized formulation, that is, xanthan gum, shows high viscosity than other viscosity modifiers. Hence, precorneal residence time of ophthalmic formulation containing xanthan gum is more. This occurs due to hydrogen bonding and polymer entanglement. Highly ordered network of entangled, stiff molecules results in high viscosity at low shear rate [13]. At low shear rates, solutions of xanthan gum have more viscosity as compared to guar gum, sodium alginate, sodium carboxymethyl cellulose, polyvinyl alcohol, gelrite, and chitosan as shown in Figure 1 [14].


Design and Evaluation of Voriconazole Eye Drops for the Treatment of Fungal Keratitis.

Malhotra S, Khare A, Grover K, Singh I, Pawar P - J Pharm (Cairo) (2014)

Comparative rheological studies of voriconazole ophthalmic formulations containing different viscosity modifiers. Values are mean ± SE of 3 in each group. PVA refers to polyvinyl alcohol, CS refers to chitosan, GG refers to guar gum, SA refers to sodium alginate, SCMC refers to sodium carboxymethyl cellulose, and XG refers to xanthan gum and gelrite.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590801&req=5

fig1: Comparative rheological studies of voriconazole ophthalmic formulations containing different viscosity modifiers. Values are mean ± SE of 3 in each group. PVA refers to polyvinyl alcohol, CS refers to chitosan, GG refers to guar gum, SA refers to sodium alginate, SCMC refers to sodium carboxymethyl cellulose, and XG refers to xanthan gum and gelrite.
Mentions: All the ophthalmic formulations containing different viscosity modifiers show pseudo plastic behavior, that is, high viscosity at low shear rate and low viscosity at high shear rate. The optimized formulation, that is, xanthan gum, shows high viscosity than other viscosity modifiers. Hence, precorneal residence time of ophthalmic formulation containing xanthan gum is more. This occurs due to hydrogen bonding and polymer entanglement. Highly ordered network of entangled, stiff molecules results in high viscosity at low shear rate [13]. At low shear rates, solutions of xanthan gum have more viscosity as compared to guar gum, sodium alginate, sodium carboxymethyl cellulose, polyvinyl alcohol, gelrite, and chitosan as shown in Figure 1 [14].

Bottom Line: The results revealed that voriconazole drop containing PVA provided least viscosity and higher corneal permeation of drug, while drop formulated with XG had maximum viscosity and least permeation.The microbiological studies showed that voriconazole ophthalmic solution containing xanthan gum shows better antifungal activity as compared to voriconazole and xanthan gum alone.Thus, it can be concluded that HP-β-CD based voriconazole (1.5%, pH 7.0) ophthalmic solution containing BAK and EDTA with viscosity modifier XG provided maximum precorneal residence time as compared to other viscosity modifiers and polyvinyl alcohol provided less precorneal residence time than other viscosity modifiers.

View Article: PubMed Central - PubMed

Affiliation: Chitkara College of Pharmacy, Chitkara University, Chandigarh-Patiala National Highway, Rajpura, Patiala, Punjab, 140401, India.

ABSTRACT
Voriconazole is a novel antifungal agent with excellent broad spectrum activity commercially available for oral and intravenous administration. The purpose of this study was to prepare ophthalmic formulation of hydroxypropyl beta cyclodextrin (HP-β-CD) based voriconazole containing benzalkonium chloride BAK and EDTA with or without viscosity modifiers and study its permeation characteristics through freshly excised goat cornea. The results were observed that viscosity and force of bioadhesion of the voriconazole HP-β-CD solutions containing xanthan gum (XG) are more as compared to polyvinyl alcohol. The results revealed that voriconazole drop containing PVA provided least viscosity and higher corneal permeation of drug, while drop formulated with XG had maximum viscosity and least permeation. The HP-β-CD based voriconazole (1.5%) ophthalmic formulation containing xanthan gum (1.5), preserved with BAK and EDTA, could provide shelf life of 2 years. The microbiological studies showed that voriconazole ophthalmic solution containing xanthan gum shows better antifungal activity as compared to voriconazole and xanthan gum alone. Thus, it can be concluded that HP-β-CD based voriconazole (1.5%, pH 7.0) ophthalmic solution containing BAK and EDTA with viscosity modifier XG provided maximum precorneal residence time as compared to other viscosity modifiers and polyvinyl alcohol provided less precorneal residence time than other viscosity modifiers.

No MeSH data available.


Related in: MedlinePlus