Abstract
Problem statement: Ophthalmic drug delivery system has been a major challenge due to the distinctive and unique anatomy of the eye. The use of phytochemicals for the application in ocular disease has not been investigated much, due to poor pharmacokinetics of phytochemical and hence poor therapeutic efficacy. Approach: Curcumin is one such phytochemical known for its medicinal properties, but its usage has been limited due to its poor bioavailability. Therapeutic ocular application of curcumin for indications such as allergic conjunctivitis and use of nanotechnology based delivery system for increasing its bioavailability haven’t been explored much. Thus the objective of current study was to develop a nanoemulsification based formulation for curcumin with enhanced bioavailability and efficacy for ophthalmic therapeutic application. Different surfactants and oils were screened based on its ability to solubilize hydrophobic curcumin for developing formulation. Ultrasonication was used for dispersion of curcumin in surfactants and nanoemulsification. Charecterization of the selected formulation was done based on particle size, Transmission Electron Microscope (TEM) and Scanning Electron Microscope (SEM) analysis and tested for different physiochemcial properties. Results: A novel formulation was developed through nanoemulsification technology by ultrasonication using carefully selected nonionic surafactants. Acconon and Tween 80 were chosen after thorough screening studies. The ratio of curcumin: Acconon: Tween80: water (0.12:1:7:1) was found to be optimum for the formulation. Particle size analysis showed that the nano droplets are in the range of 8-22 nm. Further the TEM and SEM studies also confirmed that the nanodroplets are in spherical shape. Formulation was found to be stable as ascertained by phase separation and observational studies. Conclusion: The studies ensured the stability and formation of characteristic nanodroplets with curcumin entrapment as a result of the developed formulation. The so developed formulation is expected to have higher ophthalmic bioavailability, which further needs to be confirmed through in vitro and in vivo studies.
Highlights
Drug delivery to the eye is hampered by anatomical factors, including the corneal epithelium, the bloodaqueous barrier and the blood-retinal barrier (Gaudana et al, 2010)
Designing a drug delivery system to target a particular tissue of the eye has become a major challenge for scientists in the field (Vincent et al, 1986; Abu-Al-Basalc, 2009)
Formulations of diverse types were employed to increase the aqueous solubility of curcumin thereby improving its bioavailability and pharmacokinetic properties.Addition of piperine (Shoba et al, 1998), microemulsions (Cuia et al, 2009; Shaikha et al, 2009), nanotechnological processes like nanoemulsions (Wang et al, 2008) and than smaller particles (Ratke and Voorhees, 2002)
Summary
Drug delivery to the eye is hampered by anatomical factors, including the corneal epithelium, the bloodaqueous barrier and the blood-retinal barrier (Gaudana et al, 2010). Formulations of diverse types were employed to increase the aqueous solubility of curcumin thereby improving its bioavailability and pharmacokinetic properties.Addition of piperine (Shoba et al, 1998), microemulsions (Cuia et al, 2009; Shaikha et al, 2009), nanotechnological processes like nanoemulsions (Wang et al, 2008) and than smaller particles (Ratke and Voorhees, 2002). This stems from the fact that molecules on the surface of a particle are energetically less stable than the ones in the interior.
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