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52 March 2016 Tablets & Capsules Softgels are a well-known means to enhance bioavailability and to deliver liquid APIs. Less well known is that softgels enable pharmaceutical scientists to overcome many other formulation and manufacturing chal- lenges. Softgels can also be tailored to meet the unique demands of dif- ferent markets. History and innovation It's been nearly 80 years since Robert P. Scherer invented the rotary die encapsulation process for manufac- turing soft gelatin capsules. Yet that process is the mainstay of today's com- mercial softgel manufacturing. One big advantage of softgel technology is its simplicity, which reduces develop- ment activity compared to tablets and powder-filled capsules. Those dosage forms often require changes in scale or process equipment, and those changes can have a major impact on product quality or performance. But softgel technology minimizes scaling issues because the majority of softgel fills are solutions and thus readily scale up with little impact on product quality or performance. Formulators and developers can also avoid lengthy and complex process development studies by using softgel technology, thereby eliminating surprises during late-stage development and significant delays during product development. The softgel manufacturing process also enables you to produce small batches during early development when little API is available. In fact, it's possible to manufacture batches of just a few dozen capsules for use in prob- ing stability or conducting first-in- human studies. Furthermore, you can be confident that the softgels will per- form similarly when the process is scaled up. Non-gelatin shells, such as Opti- Shell, expand the utility of softgel technology by eliminating the poten- tial for crosslinking. That enables for- mulators to use a larger variety of excipients and allows the encapsula- tion process to operate at higher tem- peratures. Formulating macromolecules and potent compounds By incorporating an enteric coating and permeation enhancers, softgels have the potential to deliver macro- molecules, such as peptides and pro- teins. The enteric coating protects the softgels from degradation in the stom- ach's acidic environment. Next, a per- meation enhancer can open up the tight junctions in the intestine and allow the macromolecules to be absorbed into the bloodstream. OptiGel Bio is one delivery vehicle under development for this purpose. Functional softgel coatings can also modify the release of APIs and enhance stability. In addition, softgels allow precise, accurate dosing of APIs at the nanogram level and often offer the best way to achieve acceptable dose uniformity of highly potent com- pounds. Furthermore, softgels offer superior containment of potent com- pounds compared to powder-based tablets and capsules, which are made using dust-prone processes. Winning consumer acceptance Other softgel benefits include rapid onset of action, ease of swal- lowing, and elegance. These charac- teristics make it the preferred dosage form of many OTC products and explain why OTC products such as analgesics and cough/cold products can command a higher price when formulated as softgels. The low oxygen permeability of softgel shells, their hermetic seal, and minimal exposure of the API to air during manufacture make softgels an excellent choice for oxygen-sensitive materials such as fish oils, vitamin D analogs, and retinoids. Plus, softgels can take nearly any shape and color to provide trademark branding, util- ity, and product differentiation. Twist-off softgels are used in cos- metic products to provide a unique and elegant unit-dose delivery sys- tem for skin and facial products. Improving animal health Softgels are also used to improve animal health. One example is SavorGel technology, which imparts desirable flavors to soft chewable capsules, leading to better accep- tance by companion animals and bet- ter therapeutic compliance. Other applications in animal health include topical administration of encapsu- lated doses of parasiticides to live- stock. Delivered via air gun, these softgels greatly reduce the labor needed to treat herds. Softgels also encapsulate orally administered vac- cines to make baits more attractive to wildlife and thereby better control diseases that threaten public health. In summary, softgels help overcome formulation challenges, serve as cus- tomized delivery containers, reduce development costs, and increase prod- uct performance and customer accep- tance in a variety of different market segments T&C David Fulper is director of technology support at Catalent Pharma Solu- tions, 2725 Scherer Drive, St. Petersburg, FL. Tel. 727 803 2178. Website: www.catalent.com. b a c k p a g e Softgels: Overcoming formulation challenges and winning customer acceptance