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In an effort to compare the performance of fully dense IVRs with foam constructs, a durometer medical-grade liquid silicone rubber LSR was premixed with Rhodamine B.

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Rings were molded via injection molding and weighed a day after molding to ensure cure and off-gassing was complete. Each ring had approximately 1. For the foam rings, the rhodamine B was mixed into the B component of the two-part foam system and made using a similar transfer press procedure. Dimensions and drug loading were similar between foamed and unfoamed systems. Rings were then suspended in 1 L of deionized water. A small weight was attached to the bottom of each ring to keep it submerged. The rings were maintained at room temperature and stirred at RPM. Samples for quantitation of elution were taken periodically, and concentration was determined using UV-VIS Spectrometry.

Figure 4 shows a photo sequence of rhodamine diffusing from a foam ring in a simple petri dish over several days. The high solubility of rhodamine is evidenced when the in vitro release of the fully dense and foam silicone IVRs are compared Figure 5. The rates are nearly identical suggesting that porosity is a secondary factor in determining the release when diffusion and dissolution into surrounding media are not rate-controlling steps.

The release behavior, however, is quite different for the two materials when a more hydrophobic small molecule is utilized. Figure 6 compares the release of Ibuprofen in silicone foams with two different densities and the same percentage drug loading. Here, the effect of water ingress on drug release is much more apparent. A greater number of pores, or larger pores present with lower density foams, allow for more surface area for water to contact the drug. Incorporation of a dissolution enhancer, such as methyl cellulose, can further increase water uptake, pore interconnectedness, and the subsequent release rate of these more hydrophobic drugs.

Finally, release of a model protein, bovine serum albumin BSA was evaluated. A controlled quantity of both silicone parts was combined in a ratio through a static mixer into a heated mold and cured. Additional samples were prepared by mixing BSA into liquid silicone rubber without use of a foaming agent and by soaking a preformed ring in a BSA solution followed by freeze drying. BSA elution for the different preparation conditions is shown in Figure 7. For post-loaded foams burst release was observed from h followed by much lower release rates.

Pre-loaded BSA foams exhibited a slower but more linear release behavior while un-foamed fully dense silicone effectively binds the BSA within the matrix, completely blocking release. By controlling loading and ring pore volume through compounding and molding, facile control of water permeation and payload release rate is possible.

Foamed silicone is capable of sustained, controlled elution of hydrophobic small molecule and large macromolecular payloads. DOI : Sterically hindered esters or esters of drugs with macromolecular carriers like dextran and cyclodextrin find wide applicability in colon-targeted delivery. In vitro stability and release were studied in buffers pH 1. The prodrug resisted pH-dependent hydrolysis. The histological assessment of pancreas and liver of the prodrug-treated group showed no pathological changes indicating its better safety profile than that of sulfasalazine or oral 5-ASA.

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Breakthrough in macromolecular machines | Times Higher Education (THE)

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Macromolecular Drug Delivery

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Exceedingly higher co-loading of curcumin and paclitaxel onto polymer-functionalized reduced graphene oxide for highly potent synergistic anticancer treatment. Sci Rep. Cutler DM.


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