Abstract
The objective of this work was to design and characterize liquid and solid self-emulsifying drug delivery systems (SEDDS) for poorly soluble atorvastatin. To optimize the composition of liquid atorvastatin-SEDDS, solubility tests, pseudoternary phase diagrams, emulsification studies and other in vitro examinations (thermodynamic stability, droplet size and zeta potential analysis) were performed. Due to the disadvantages of liquid SEDDS (few choices for dosage forms, low stability and portability during the manufacturing process), attempts were also made to obtain solid SEDDS. Solid SEDDS were successfully obtained using the spray drying technique from two optimized liquid formulations, CF3 and OF2. Despite liquid SEDDS formulation, CF3 was characterized by lower turbidity, higher percentage transmittance and better self-emulsifying properties, and based on the in vitro dissolution study it can be concluded that better solubilization properties were exhibited by solid formulation OF2. Overall, the studies demonstrated the possibility of formulating liquid and solid SEEDS as promising carriers of atorvastatin. SEDDS, with their unique solubilization properties, provide the opportunity to deliver lipophilic drugs to the gastrointestinal tract in a solubilized state, avoiding dissolution—a restricting factor in absorption rate of BCS Class 2 drugs, including atorvastatin.
Highlights
The majority of new drugs exhibit poor aqueous solubility, which affects their low bioavailability after oral delivery
self-emulsifying drug delivery systems (SEDDS) are isotropic mixtures of oils and surfactants with or without co-surfactants, which act as lipid-based formulations after oral application in aqueous gastrointestinal fluid and upon gentle agitation can form an oil-in-water emulsion [7,8,9,10]
Solid self-emulsifying drug delivery systems (S-SEDDS) could be formulated in the form of self-emulsifying capsules, pellets/tablets, micro/nano-particles, suppositories or dry emulsions
Summary
The majority of new drugs exhibit poor aqueous solubility, which affects their low bioavailability after oral delivery. A relatively new approach for poorly soluble drugs is lipid-based formulations, self-emulsifying drug delivery systems (SEDDS) [5,6]. SEDDS as liquid formulations have several disadvantages such as low drug loading capacity, drug leakage, low stability, and few choices of dosage forms. To overcome these limitations, liquid SEDDS (L-SEDDS) can be transformed to solid dosage forms by using different methods (filling capsules with liquid or semi-solid SEDDS, adsorption to solid carrier, melt granulation, spray drying, melt extrusion or nanoparticle formation) [15,16]. This technique allows preparation of the self-emulsifying dry emulsion by removing water from an emulsion containing a water-soluble solid carrier [19,20,21]
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
