Ultrasonically Formulated Famotidine Solid-Lipid Nanoparticles
Famotidine is a common pharmaceutical molecule used in heartburn medications. In order to overcome the poor solubility and the resulting poor bioavailability, famotidine can be formulated into solid-lipid nanoparticles using sonication as encapsulation technique.
Ultrasonically Famotidine-Loaded Solid Lipid Nanoparticles
Sonication is widely used in the production of pharmaceuticals, vaccines and dietary supplements. An important application is the formulation, encapsulation and/or entrapment of bioactive molecules (i.e. drug substance) into nano-structured functional drug delivery systems such as solid-lipid nanoparticles, liposomes, niosomes, inclusion complexes or polymeric nanoparticles.
Famotidine is an H2 receptor blocker and the active compound in the widely used over-the-counter (OTC) heartburn drug Pepcid. Absorption orally is rapid enough, but famotidine can be degraded by stomach acid causing dose reduction until 35.8% after 50 minutes. This drug also undergoes first-pass metabolism which reduced its bio availability only until 40-50%
As of end of April 2020, famotidine is also studied as potential drug to treat patients suffering from the SARS-CoV-2 (coronavirus) caused COVID-19 disease. In a clinical trial, patients with severe coronavirus disease COVID-19 are receiving famotidine intravenously.
Common famotidine containing drugs are known under various brand names such as Pepcid AC, Acid Controller, Pepcid, Acid Reducer (famotidine), Heartburn Prevention, and Heartburn Relief (famotidine).
Ultrasonic Preparation of Solid-Lipid Nanoparticles
The ultrasonic preparation of famotidine-loaded solid lipid nanoparticles (SLNs) is a simple and efficacious technique to formulate a high-quality nano-sized drug delivery system with significantly increased bioavailability.
Zai et al. (2019) prepared solid lipid nanoparticles (SLNs) using the ultrasonically-assisted hot emulsification technique. Glyceryl monostearate and Span 20 (3:1 w/w) mixture were melted at approx. 60°C and added famotidine (2 mg/mL of total vol.). Water containing poloxamer (4mg/mL) was heated also at approx. 60°C and transferred to the molten lipid mixture. The lipid and aqueous phase were mixed by high-shear homogenizer at 5,000 rpm for 5 min, then sonicated with a probe-type ultrasonicator for 5 min.
The results showed that the famotidine-loaded solid lipid nanoparticles had a mean particle size of an average 151,90 ± 26,05 nm and a relatively small size distribution (0,35 ± 0,04). The famotidine-loaded solid lipid nanoparticles had a high entrapment efficiency of 82,30 ± 4,39 % and an increased bioavailability.
- High performance emulsification
- Simple, efficient encapsulation
- High loading of bioactive molecules
- Exact control over process parameters
- Fast Process
- Non-thermal, precise temp control
- Linear Scalability
- Process standardisation / GMP
- Autoclavable probes and reactors
- CIP / SIP
High-Performance Ultrasonicators for Pharma Formulations
Hielscher Ultrasonics is long-time experienced in the design, manufacturing, distribution and service of high-performance ultrasonic homogenisers for the pharmaceutical and food industry.
The preparation of high-quality solid lipid nanoparticles, nanostructured lipid carriers, liposomes, niosomes, and cyclodextrin inclusion complexes are processes, which Hielscher ultrasonic systems are used with high reliability and superior quality output. Hielscher ultrasonicators allow for precise control over all process parameters, such as amplitude, temperature, pressure and sonication energy. The intelligent software automatically protocols all sonication parameters (time, date, amplitude, net energy, total energy, temperature, pressure) on the built-in SD-card.
The table below gives you an indication of the approximate processing capacity of our ultrasonicators:
|Batch Volume||Flow Rate||Recommended Devices|
|1 to 500mL||10 to 200mL/min||UP100H|
|10 to 2000mL||20 to 400mL/min||UP200Ht, UP400St|
|0.1 to 20L||0.2 to 4L/min||UIP2000hdT|
|10 to 100L||2 to 10L/min||UIP4000hdT|
|n.a.||10 to 100L/min||UIP16000|
|n.a.||larger||cluster of UIP16000|
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Literature / References
- Khadijah Zai, Rachmat Mauludin, Diky Mudhakir (2019): Solid Lipid Nanoparticle Improves Oral Bioavailability of Famotidine. J. Pharm. Sci. & Res. Vol. 11(6), 2019. 2437-2439.
- Rachmat Mauludin, Nurmazidah (2014): Formulation of Famotidine Solid Lipid Nanoparticles (SLN): Preparation, Evaluation and Release Study. International Conference on Pharmacy and Pharmacology, Bangkok, Thailand. December 18-19, 2014.
- Eszter L. Kiss, Szilvia Berkó, Attila Gácsi, Anita Kovács, Gábor Katona, Judit Soós, Erzsébet Csányi, Ilona Gróf, András Harazin, Mária A. Deli, Mária Budai-Szűcs (2019): Design and Optimization of Nanostructured Lipid Carrier Containing Dexamethasone for Ophthalmic Use. Pharmaceutics. 2019 Dec; 11(12): 679.
Facts Worth Knowing
Nanocarriers for Drug Delivery
A nanocarrier is nanomaterial being used as a transport module for another substance, such as a drug. Commonly used nanocarriers include micelles, polymers, core-shell nanoparticles, liposomes, dendrimers, solid-lipid nanoparticles and nanostructured lipid carriers. One of the main advantages of nanocarriers is their minute size which enables them to penetrate cells and to deliver the loaded active substance into the targeted tissue. Being able to modify physical properties of the nanocarriers, e.g. shape, composition and size, nanocarriers can be functionalized specifically to certain therapeutic agents and drug release patterns.