Lindmik Research I Cyclodextrin Ibuprofen Electrospinning Oral Soluble Membrane
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The poor water solubility of candidate drugs poses a significant challenge for pharmaceutical scientists to achieve effective oral administration. Poor solubility is often associated with poor dissolution behavior, which in turn results in poor bioavailability of such drugs when intestinal absorption is limited by dissolution rates. The poor solubility and low dissolution rate of ibuprofen (IBU) in gastrointestinal aqueous solutions limit its application, absorption, distribution, target organ delivery, and bioavailability. In recent years, multiple research teams across the country have attempted to develop electrospun polymer nanofibers to solve the problem of poor water solubility of ibuprofen, a class II drug in the Biological Pharmaceutical Classification System (BCS). Hydrophilic spinnable polymers such as cyclodextrins, cellulose acetate, vinyl pyrrolidone, and polycaprolactone are used as carrier systems for the manufacture of nanofibers. Scientists are trying to optimize electrospinning parameters such as flow rate, voltage, and the distance from the spinneret to the collector. The prepared ibuprofen loaded nanofibers were characterized and analyzed using scanning electron microscopy and differential scanning calorimetry. Drug release studies and in vitro intestinal absorption studies have also been conducted. Compared to pure ibuprofen crystals, the nanofiber based platform significantly improves the in vitro absorption of ibuprofen.


Rapidly dissolving oral membranes are often prepared from hydrophilic polymers such as gelatin, starch, and carboxymethyl cellulose (CMC), hydroxypropylcellulose (HPC), pectin, alginate, chitosan, pullulan, polyvinyl pyrrolidone (PVP), polyethylene glycol (PEO), and polyvinyl alcohol (PVA). The commonly used technology for producing rapidly dissolving oral membranes is film casting or hot melt method, which disperses active compounds and encapsulates them in hydrophilic water layers. Rapidly dissolving oral membranes should have a certain degree of mechanical integrity.

Two methods dominate film manufacturing: solvent casting (Figure 1) and hot melt extrusion (Figure 2). Both have advantages and disadvantages, depending on the nature of the API used and the characteristics required for the final product.

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Below is ibuprofen and hydroxypropyl- β- The chemical structure of cyclodextrins. Ibuprofen and hydroxypropyl- β- Schematic diagram of inclusion complex formation between cyclodextrin molecules, and hydroxypropyl group- β- Technical principle of electrospinning of cyclodextrin/ibuprofen inclusion complex nanofibers.

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The following figure (Figure 14) shows the functional electrospun nanofiber patch delivered by ibuprofen (IBU) in the oral mucosa, which is made by the Melodie Lawton team from the Hajim School of Engineering and Applied Sciences at the University of Rochester using a mixture of polycaprolactone (PCL) and polyvinylpyrrolidone (PVP). Their research found that the optimal blend for drug delivery and fiber formation is PCL: PVP with a ratio of 70:30.3


The following video shows the pure ibuprofen powder and hydroxypropyl used by the Asli Celebioglu team at Cornell University- β- Cyclodextrin/ibuprofen (1:1) and hydroxypropyl- β- Dissolution effect of electrospinning of cyclodextrin/ibuprofen (2:1) inclusion complex nanofibers in distilled water.




2.DOI: 10.1021/acs.molpharmaceut.9b00798


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