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26 March/April 2021 Tablets & Capsules taste. Also, fatty acids do not hydrolyze in the oral cavity, allowing the active to be masked effectively by flavorants and sweeteners added to the lipid formulation. Oil-based flavors are excellent for flavoring lipid-based microencapsulated products. The oil-based flavor is soluble in lipid bases, affording a smooth flavor profile capturing the flavor essence. Oil-based flavors are encapsulated within the lipid microencapsulation matrix, so the flavor profile is sustained over time. The resulting product provides desir- able organoleptic properties as well as tastes consumers enjoy and trust. Maintaining potency and preventing color migration Lipid microencapsulation can also effectively maintain potency, prevent color migration, and block unpleasant odors in dietary supplement products. Common nutrients that lose potency over time include folic acid and vitamin B12, which can lose up to 10 percent of their potency after six months, and vitamin A, which can lose 40 percent of its potency after six months [8]. Moreover, some vitamins can stain the oral cavity. For example, vitamin B2 from riboflavin transfers a yellow color, and iron vitamins from ferrous fumarate, ferrous sulfate, and polysaccharide iron complex transfer a black or brown color. Lipid microencapsulation prevents such color staining. Examples of lipid microencapsulation Examples of successfully marketed pharmaceutical prod- ucts that use lipid microencapsulation include azithromycin dihydrate, somatropin, follitropin, erythropoietin [2], acet- aminophen, and ibuprofen. Pharmaceutical active ingredi- ents have essential release and tolerance criteria established within the US Pharmacopeia (USP) monograph. For exam- ple, ibuprofen has a release tolerance of not less than 80 percent and is required to dissolve/release within 60 minutes. Figure 1 shows the release profile of marketed 50-milligram chewable ibuprofen tablets for adults and children. Figure 2 shows the release profile of marketed 100-milligram chew- of the active to react with other formulation ingredients and promotes stability. Increasing bioavailability According to a 2020 Catalent survey of more than 200 scientific researchers, lipid formulations are the primary tech- nology that researchers are currently working on for early clinical trials and provide optimal bioavailability enhance- ment for poorly soluble actives [3]. Lipids are important for improving the bioavailability of poorly soluble actives. Lipids are an integral part of the human anatomy, as they are the main components of cel- lular membranes [4]. The lipid bilayer of cell membranes is made of intracellular and extracellular components that control the passage of substances entering and exiting the cell membrane [5]. Therefore, when poorly soluble actives are formulated through lipid microencapsulation, the lipid bilayer of the cellular membrane facilitates solubilization of the lipid microencapsulated particles [6]. The solubilized phases impact the absorption of actives, increasing disso- lution of the lipid and bioavailability of the active in the intracellular and extracellular digestion process. Taste masking and flavor additives The suppression of bitter tastes in oral dosage forms is important for patient compliance. The dislike of bit- ter tasting vitamins and medications, especially among young children, may lead to suboptimal treatment [7]. Bitterness, astringency, chalkiness, and metallic tastes can be suppressed using masking agents, sweeteners, and fla- vorants. Embedding these masking agents, sweeteners, and flavorants into the lipid-active matrix masks bitter-tasting actives and makes the product more palatable, which can increase patient compliance. Lipid-based microencapsulation enhances taste masking because of the characteristics of the lipids, masking agents, and flavorants used [6]. Lipid formulations that use satu- rated long-chained biocompatible fatty acids have a neutral Figure 1 Release pro le of chewable tablet manufactured using 50 milligrams of lipid microencapsulated ibuprofen (Micromask Ibuprofen 72%) Ibuprofen released (percentage) 100 90 80 70 60 50 40 30 20 10 0 Time (minutes) 5 10 20 30 30 80 95 98 Figure 2 Release pro le of chewable tablet manufactured using 100 milligrams of lipid microencapsulated ibuprofen (Micromask Ibuprofen 72%) Time (minutes) 5 10 20 30 33 80 94 95 Ibuprofen released (percentage) 100 90 80 70 60 50 40 30 20 10 0