Creation, Profiling, and Assessment of an Innovative in-situ Gel Incorporating Doxycycline for Enhanced Ocular Drug Release

Author: Patel L.K. and Naresh Kalra

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Abstract

Aim of the present study was to design and develop in-situ gel-forming containing Doxycycline Hyclate and evaluate against dry eye disease related bacterial infections. The formulation was systemically optimized using simplex lattice design model. The optimized formulation was evaluated for clarity, pH measurement, gelling capacity, Gel strength, drug content estimation, rheological study, viscosity, in-vitro diffusion study, antimicrobial activity, and osmolality study. The Gellan gum is a well-known natural source of gel-forming mucoadhesive polymer, which gets converted to gel in the presence of divalent-cations (calcium ion) present in the lachrymal fluid, was used as the gelling agent. The optimized In-situ formulations were evaluated for osmolality 260-310 mOs mol/kg, drug content 95-100% and pH 6.5-7.4, gelling time 22 seconds, gelling strength. The antimicrobial efficacy results showed that not less than 1.0 log reduction from the initial calculated count at 7 days, not less than 3.0 log reduction from the initial calculated count at 14 days, and no increase from the 14 days count at 28 days. The obtained results indicated that the elaborated in-situ gel system containing Doxycycline Hyclate has been successfully developed. Results showed that a suitable combination of polymers Gellan gum, Povidone K30 & Hypromellose were provide better Mucoadhesion and to increase the residence time. This may be helpful in term of patient compliance for the dry eye disease related bacterial infections. This in situ gelling system containing natural source of gums may be a valuable alternative to the conventional systems.

Keywords

Dry eye disease, In-situ gel, Doxycycline Hyclate, drug delivery, polymer, Gellan gum

Conclusion

In the present study, ion responsive in-situ gel forming solution containing doxycycline Hyclate was prepared and evaluated for antimicrobial activity. Gellan gum in a concentration of 6mg/mL (0.6% w/w) showed optimum gelation when mix with simulated tear fluid (STF). Benzalkonium chloride used as a preservative which showed good preservative efficacy at a concentration of 0.05mg/mL (0.005% w/w). In situ gel forming ophthalmic solution available in market containing Timolol was used to compare the other physicochemical parameters like gel strength, gelling time, viscosity, gelling capacity with prepared in-situ gel forming solution out of that formulation R6 found satisfactory and comparable.

References

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How to cite this article

Patel L.K. and Naresh Kalra (2023). Creation, Profiling, and Assessment of an Innovative in-situ Gel Incorporating Doxycycline for Enhanced Ocular Drug Release. Biological Forum – An International Journal, 15(5a): 563-568.