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Pharmaceutical Manufacturing Handbook: Production and

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REFERENCES 785<br />

stability of incorporated drugs with potential increase in bioavailability; hence these<br />

systems could be a suitable alternative to conventional ocular formulations. So far,<br />

only few investigators [124 – 127] have considered the use of MEs for ocular drug<br />

delivery. Their work was solely focused on o/w MEs as ocular delivery carriers.<br />

Recently Alany et al. [128] reported on w/o MEs formulated using a blend of two<br />

nonionic surfactants (Crillet 4 <strong>and</strong> Crill 1), an oily component (Crodamol EO), <strong>and</strong><br />

water. These systems were shown to be capable of undergoing a phase change to<br />

lamellar liquid crystals upon aqueous dilution. The ocular irritation potential of the<br />

individual components <strong>and</strong> fi nal formulations was assessed using a modifi ed hen ’ s<br />

egg chorioallantoic membrane test (HET - CAM), <strong>and</strong> the preocular retention was<br />

investigated in the rabbit eye using gamma scintigraphy. The authors demonstrated<br />

that the retention of ME systems was signifi cantly greater than an aqueous solution.<br />

The rapid clearance of the w/o ME formulated with 10% water compared to the<br />

LC system indicated that phase change is less likely to take place in the rabbit eye<br />

[128] . It was also concluded that w/o MEs may be of value as vehicles for the ocular<br />

drug delivery of irritant hydrophilic drugs as they appear to have a protective effect<br />

when evaluated using a modifi ed HET - CAM test [128] . The potential of bicontinuous<br />

ME systems as vehicles for ocular drug delivery is yet to be investigated. A<br />

recent review reported on the potential of MEs as ocular drug delivery systems;<br />

however, submicrometer emulsions <strong>and</strong> systems requiring energy input to prepare<br />

were also covered <strong>and</strong> classifi ed as MEs [129] .<br />

5.10.7<br />

CONCLUDING REMARKS<br />

Microemulsions represent an exciting opportunity for pharmaceutical formulators<br />

<strong>and</strong> drug delivery scientists. They are easy to prepare <strong>and</strong> thermodynamically stable.<br />

Moreover, they can accommodate drugs of different physicochemical properties <strong>and</strong><br />

protect those that are labile. They have the potential to increase the solubility of<br />

poorly water soluble drugs, enhance the bioavailability of problematic drugs, reduce<br />

patient variability, <strong>and</strong> offer an option for controlled drug release. A critical look at<br />

the current literature shows that exciting <strong>and</strong> promising research is taking place. It<br />

is only a matter of time before new ME - based products will fi nd their way to the<br />

market following the successful introduction of S<strong>and</strong>immune Neoral.<br />

REFERENCES<br />

1. Danielsson , I. , <strong>and</strong> Lindman , B. ( 1981 ), The defi nition of microemulsion , Colloid Surfaces<br />

, 3 , 391 .<br />

2. Tenjarla , S. ( 1999 ), Microemulsions: An overview <strong>and</strong> pharmaceutical applications<br />

[Review] , Crit. Rev. Ther. Drug Carrier Syst. , 16 ( 5 ), 461 – 521 .<br />

3. Attwood , D. ( 1994 ), Microemulsions , in Kreuter , J. , Ed., Colloidal Drug Delivery Systems ,<br />

Marcel Dekker , New York , pp 31 – 71 .<br />

4. Lawrence , M. J. , <strong>and</strong> Rees , G. D. ( 2000 ), Microemulsion - based media as novel drug<br />

delivery systems , Adv. Drug Del. Rev. , 45 ( 1 ), 89 – 121 .<br />

5. Mitchell , D. , <strong>and</strong> Ninham , W. ( 1981 ), Micelles vesicles <strong>and</strong> microemulsions , J. Chem. Soc.<br />

Faraday Trans. , 77 ( 2 ), 601 – 629 .

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