Optimization of solid-self nanoemulsifying drug delivery system for solubility and release profile of clonazepam using simplex lattice design

Sanka, Krishna; Suda, Deepthi; Bakshi, Vasudha

doi:10.1016/j.jddst.2016.04.003

Cited by 42 publications

(20 citation statements)

References 43 publications

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“…Small increments of water were added with waiting periods in-between until the full predetermined quantity was included. The SEDDSs were left to cool before storage at room temperature (25 ± 0.5 °C) for 24 h; followed by visual observation of phase separation to identify any indication of formulation instability [ 46 , 47 , 48 ]. SEDDSs were exposed to increased temperatures during production.…”

Section: Methodsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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A quality-by-design and characterization approach was followed to ensure development of self-emulsifying drug delivery systems (SEDDSs) destined for topical delivery of the highly lipophilic clofazimine. Solubility and water-titration experiments identified spontaneous emulsification capacity of different excipient combinations and clofazimine. After identifying self-emulsification regions, check-point formulations were selected within the self-emulsification region by considering characteristics required to achieve optimized topical drug delivery. Check-point formulations, able to withstand phase separation after 24 h at an ambient temperature, were subjected to characterization studies. Experiments involved droplet size evaluation; size distribution; zeta-potential; self-emulsification time and efficacy; viscosity and pH measurement; cloud point assessment; and thermodynamic stability studies. SEDDSs with favorable properties, i.e., topical drug delivery, were subjected to dermal diffusion studies. Successful in vitro topical clofazimine delivery was observed. Olive oil facilitated the highest topical delivery of clofazimine probably due to increased oleic acid levels that enhanced stratum corneum lipid disruption, followed by improved dermal clofazimine delivery. Finally, isothermal microcalometric experiments studied the compatibility of excipients. Potential interactions were depicted between argan oil and clofazimine as well as between Span®60 and argan-, macadamia- and olive oil, respectively. However, despite some mundane incompatibilities, successful development of topical SEDDSs achieved enhanced topical clofazimine delivery.

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Section: Methodsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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“…In addition to a ternary phase diagram, SNEDDSs optimization can also be done with numerous types of statistical experimental design, such as Box–Benkhen design [ 50 , 51 , 52 ], central composite design [ 53 ], simplex lattice design [ 54 ], full-factorial design [ 55 ], and D-optimal design [ 56 ].…”

Section: Optimization Of Sneddss Formulationsmentioning

confidence: 99%

“…Differential scanning calorimetry (DSC) and thermal gravimetric analysis (TGA) are mostly used to evaluate the thermal behavior of solid SNEDDSs. In these techniques, samples are subjected to heating at a specified temperature rate under different atmospheres such as argon, oxygen, and nitrogen [ 54 ]. The main information generated from these techniques is the melting point, crystallinity, polymorphism, and endothermic and exothermic behaviors of the sample, which are related to a reference standard [ 283 ].…”

Section: Advancements In Sneddssmentioning

confidence: 99%

Self-Nano-Emulsifying Drug-Delivery Systems: From the Development to the Current Applications and Challenges in Oral Drug Delivery

et al. 2020

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Approximately one third of newly discovered drug molecules show insufficient water solubility and therefore low oral bio-availability. Self-nano-emulsifying drug-delivery systems (SNEDDSs) are one of the emerging strategies developed to tackle the issues associated with their oral delivery. SNEDDSs are composed of an oil phase, surfactant, and cosurfactant or cosolvent. SNEDDSs characteristics, their ability to dissolve a drug, and in vivo considerations are determinant factors in the choice of SNEDDSs excipients. A SNEDDS formulation can be optimized through phase diagram approach or statistical design of experiments. The characterization of SNEDDSs includes multiple orthogonal methods required to fully control SNEDDS manufacture, stability, and biological fate. Encapsulating a drug in SNEDDSs can lead to increased solubilization, stability in the gastro-intestinal tract, and absorption, resulting in enhanced bio-availability. The transformation of liquid SNEDDSs into solid dosage forms has been shown to increase the stability and patient compliance. Supersaturated, mucus-permeating, and targeted SNEDDSs can be developed to increase efficacy and patient compliance. Self-emulsification approach has been successful in oral drug delivery. The present review gives an insight of SNEDDSs for the oral administration of both lipophilic and hydrophilic compounds from the experimental bench to marketed products.

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“…Additionally, capsule technologies have some limitations such as high production cost and the risk of interaction between the active pharmaceutical ingredient and excipients with the capsule shell. Also, the possibility of drug leakage out of the capsule shell and capsule aging represent further obstacles [76]. Further, the storage temperature is an important consideration since the drug and/or excipients could undergo precipitation at lower temperatures [75].…”

Section: Solid Self-emulsifying Drug Delivery Systemsmentioning

confidence: 99%

“…FT-IR is usually employed to investigate any potential interaction between the incorporated drug and the solid carrier or other formulation excipients [76].…”

Section: Fourier-transform Infrared Spectroscopy (Ft-ir)mentioning

confidence: 99%

Self-Emulsifying Drug Delivery Systems: Easy to Prepare Multifunctional Vectors for Efficient Oral Delivery

AboulFotouh¹,

Allam²,

El-Badry³

2020

Current and Future Aspects of Nanomedicine

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Self-emulsifying drug delivery systems (SEDDS) have been mainly investigated to enhance the oral bioavailability of drugs belonging to class II of the Biopharmaceutics Classification System. However, in the past few years, they have shown promising outcomes in the oral delivery of various types of therapeutic agents. In this chapter, we discuss the recent progress in the application of SEDDS for oral delivery of protein therapeutics and genetic materials. The role of SEDDS in enhancing the oral bioavailability of P-glycoprotein and cytochrome P450 3A4 substrate drugs is also highlighted. Also, we discuss the most critical evaluation criteria of SEDDS. Additionally, we summarize various solidification techniques employed to transform liquid SEDDS to the more stable solid self-emulsifying drug delivery systems (s-SEDDS) that are associated with high patient compliance. This chapter provides a comprehensive approach to develop high utility SEDDS and their further transformation into s-SEDDS.

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Optimization of solid-self nanoemulsifying drug delivery system for solubility and release profile of clonazepam using simplex lattice design

Cited by 42 publications

References 43 publications

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Self-Nano-Emulsifying Drug-Delivery Systems: From the Development to the Current Applications and Challenges in Oral Drug Delivery

Self-Emulsifying Drug Delivery Systems: Easy to Prepare Multifunctional Vectors for Efficient Oral Delivery

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