Naringenin (NRG), predominant flavanone in grapefruits, possesses anti-inflammatory, anti-carcinogenic, hepato-protective and anti-lipid peroxidation effects. Slow dissolution after oral ingestion due to its poor solubility in water, as well as low bioavailability following oral administration, restricts its therapeutic application. The study is an attempt to improve the solubility and bioavailability of NRG by employing self-nanoemulsifying drug delivery technique. Preliminary screening was carried out to select oil, surfactant and co-surfactant, based on solubilization and emulsification efficiency of the components. Pseudo ternary phase diagrams were constructed to identify the area of nanoemulsification. The developed self-nanoemulsifying drug delivery systems (SNEDDS) were evaluated in term of goluble size, globule size distribution, zeta potential, and surface morphology of nanoemulsions so obtained. The TEM analysis proves that nanoemulsion shows a droplet size less than 50 nm. Freeze thaw cycling and centrifugation studies were carried out to confirm the stability of the developed SNEDDS. In vitro drug release from SNEDDS was significantly higher (p < 0.005) than pure drug. Furthermore, area under the drug concentration time-curve (AUC(0-24)) of NRG from SNEDDS formulation revealed a significant increase (p < 0.005) in NRG absorption compared to NRG alone. The increase in drug release and bioavailability as compared to drug suspension from SNEDDS formulation may be attributed to the nanosized droplets and enhanced solubility of NRG in the SNEDDS.
Polymeric micelles (PMs) have made significant progress in drug delivery applications. A robust core–shell structure, kinetic stability and the inherent ability to solubilize hydrophobic drugs are the highlights of PMs. This review presents the recent advances and understandings of PMs with a focus on the latest drug delivery applications. The types, methods of preparation and characterization of PMs are described along with their applications in oral, parenteral, transdermal, intranasal and other drug delivery systems. The applications of PMs for tumor-targeted delivery have been provided special attention. The safety, quality and stability of PMs in relation to drug delivery are also provided. In addition, advanced polymeric systems and special PMs are also reviewed. The in vitro and in vivo stability assessment of PMs and recent understandings in this area are provided. The patented PMs and clinical trials on PMs for drug delivery applications are considered indicators of their tremendous future applications. Overall, PMs can help overcome many unresolved issues in drug delivery.
There is lot of confusion in the literatures regarding the method of production of nanoemulsion. According to some authors, only the methods using high energy like high-pressure microfluidizer or high-frequency ultra-sonic devices can produce actual nanoemulsions. In contrast to this concept, one research group reported for the first time the preparation of nanoemulsion by a low-energy method. Later on many authors reported about the low-energy emulsification method. The purpose of this work is to formulate, evaluate and compare nanoemulsions prepared using high-energy as well as low-energy method. Nanoemulsions formulated were based on the phase inversion composition technique (low energy method) and were selected from the ternary phase diagram based on the criterion of their being a minimum concentration of Smix used in the formulation. For high-pressure homogenization method (high energy method) Design-Expert software was used, and the desirability function was probed to acquire an optimized formulation. No significant difference (p > 0.05) was observed in the globule size of formulations made by each method, but the value of poly-dispersibility index between the two methods was found to be extremely significant (p < 0.001). A very significant difference (p < 0.001) was observed in the drug release from formulations made by each method. More than 60% of the drug was released from all the formulations in the initial 2 h of the dissolution study.
Introduction : More than 40% of new chemical entities discovered are poorly water soluble and suffer from low oral bioavailability. In recent years, nanoemulsions are receiving increasing attention as a tool of delivering these low-bioavailable moieties in an efficient manner. Areas covered : This review gives a brief description about how oral nanoemulsions act as a tool to improve the bioavailability of poorly water-soluble drugs. The recurrent confusion found in the literature regarding the theory behind the formation of nanoemulsions is clarified, along with the difference between nanoemulsion and lyotropic ‘microemulsion' phase. This paper gives a clear-cut idea about all possible methods for the preparation of nanoemulsions and the advantages and disadvantages of each method are described. A description of the stability problems of nanoemulsions and their prevention methods is also provided, in addition to a comprehensive update on the patents and research works done in the arena of oral nanoemulsions. Expert opinion : Low-energy emulsification techniques can also produce stable nanoemulsions. It is guaranteed that oral nanoemulsions can act as a potential tool for the delivery of poorly water-soluble therapeutic moieties in a very efficient manner.
Background: 3D printing technology is a new chapter in pharmaceutical manufacturing and has gained vast interest in the recent past as it offers significant advantages over traditional pharmaceutical processes. Advances in technologies can lead to the design of suitable 3D printing device capable of producing formulations with intended drug release. Methods: This review summarizes the applications of 3D printing technology in various drug delivery systems. The applications are well arranged in different sections like uses in personalized drug dosing, complex drugrelease profiles, personalized topical treatment devices, novel dosage forms and drug delivery devices and 3D printed polypills. Results: This niche technology seems to be a transformative tool with more flexibility in pharmaceutical manufacturing. Typically, 3D printing is a layer-by-layer process having the ability to fabricate 3D formulations by depositing the product components by digital control. This additive manufacturing process can provide tailored and individualized dosing for treatment of patients different backgrounds with varied customs and metabolism pattern. In addition, this printing technology has the capacity for dispensing low volumes with accuracy along with accurate spatial control for customized drug delivery. After the FDA approval of first 3D printed tablet Spritam, the 3D printing technology is extensively explored in the arena of drug delivery. Conclusion: There is enormous scope for this promising technology in designing various delivery systems and provides customized patient-compatible formulations with polypills. The future of this technology will rely on its prospective to provide 3D printing systems capable of manufacturing personalized doses. In nutshell, the 3D approach is likely to revolutionize drug delivery systems to a new level, though need time to evolve.