Abstract
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The current review focuses on the advantages offered by a cationic submicronic oil-in-water emulsion over conventional formulations in delivering a poorly soluble drug to eye. The submicronic oil globules in a cationic oil-in-water emulsion act as vectors for poorly-soluble drug to eye. The positively charged oil globules are electrostatically attracted to the negatively charged conjunctival mucous membrane.The drug uptake occurs by receptor-mediated endocytosis of the cationic oil globules.The drug shows a controlled release by above mechanism. This phenomenon aids in decreasing the frequency of administration of the formulation and enhancing patient-compliance. The aqueous phase of oil-in-water emulsion can also be utilized to target a water- soluble drug. The submicronic size of oil globules aid in enhanced stability profile of the emulsion. Furthermore the lowered size of the globules makes the formulation non-irritant to the delicate ocular surface. The use of non-toxic, non-irritant surfactant systems to emulsify the oil aids in lowering the surface tension of the aqueous phase thus increasing the wetting of the ocular surface by the formulation. The formulation approach comprises of applying a synergism of stirring along with high speed homogenisation or high pressure homogenisation to give the desirable submicronic globule size. Medium chain triglycerides (most preferred oil phase) are stabilized in the aqueous phase by utilizing a combination of non-ionic surfactants (Poloxamers, Polysorbates, etc) and cationic lipids(Stearylamine, Oleylamine etc). Miscellaneous additives like preservatives, tonicity modifiers and viscosity modifiers can be added to impart the system with enhanced ocular compatibility.The emulsion stability depends on the formulation method, nature of cationic lipid and the aqueous phase composition. The emulsion formulation when delivered in the form of eyedrops provides a patient-friendly means of delivering a poorly-soluble drug to the anterior as well as the posterior segment of the eye. |
