2018
DOI: 10.1039/c8ra02588f
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Poly(allylamine)/tripolyphosphate coacervates enable high loading and multiple-month release of weakly amphiphilic anionic drugs: an in vitro study with ibuprofen

Abstract: Gel-like coacervates prepared through ionotropic gelation enable very high loading and multiple-month release of weakly amphiphilic small molecules. Conversely, strong amphiphile incorporation disrupts ionic crosslinking and strikingly alters the coacervate properties.

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Cited by 20 publications
(28 citation statements)
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References 51 publications
(123 reference statements)
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“…The moderate increase in swelling of the payload-free coacervates when placed in water was consistent with those previously reported for both PAH/TPP networks , and polyelectrolyte complex coacervates (prepared through the mixing of oppositely charged polymers). , Moreover, the increase in swelling with the coacervate loading was qualitatively similar to that seen in prior work upon the encapsulation of a nonbinding zwitterionic dye (Rhodamine B) . Because the LCs with the dye molecules were orders of magnitude lower than those used here, however, the swelling in that earlier work was much more modest (with the coacervate weights changing by just 10–30% when placed in deionized water or phosphate-buffered saline) .…”
Section: Resultssupporting
confidence: 89%
See 1 more Smart Citation
“…The moderate increase in swelling of the payload-free coacervates when placed in water was consistent with those previously reported for both PAH/TPP networks , and polyelectrolyte complex coacervates (prepared through the mixing of oppositely charged polymers). , Moreover, the increase in swelling with the coacervate loading was qualitatively similar to that seen in prior work upon the encapsulation of a nonbinding zwitterionic dye (Rhodamine B) . Because the LCs with the dye molecules were orders of magnitude lower than those used here, however, the swelling in that earlier work was much more modest (with the coacervate weights changing by just 10–30% when placed in deionized water or phosphate-buffered saline) .…”
Section: Resultssupporting
confidence: 89%
“…Recently, one of us hypothesized that highly sustained disinfection could be achieved using putty-like complex coacervates formed from aqueous mixtures of the cationic polymer, poly­(allylamine hydrochloride) (PAH), and pentavalent anion, tripolyphosphate (TPP) (see Scheme a,b) . These coacervates can both adhere to diverse surfaces , and release small molecules over multiple months. , The long-term sustained release functionality of PAH/TPP coacervates likely reflects their high network densities and has, to date, been demonstrated using water-soluble (anionic and zwitterionic) dyes and the anti-inflammatory drug ibuprofen . Besides their adhesion and long-term release functionalities, PAH/TPP coacervates have shown promising cytocompatibilities with human cells, which suggests these materials to be relatively nontoxic .…”
Section: Introductionmentioning
confidence: 99%
“…Previously, Lapitsky and coworkers observed this reduction in cross‐link density induced by salt effects in gel‐like coacervates prepared from the ionic self‐assembly of PAH with either pyrophosphate or tripolyphosphate . On the other hand, these gels showed a high capacity to encapsulate small molecules and release them over multiple‐month timescales . The slow release rate is possibly due to a higher cross‐link density generated by the use of ionic cross‐linkers with higher net charge as compared to single phosphate.…”
Section: Resultsmentioning
confidence: 96%
“…To ensure that amino groups remain un‐ionized, experiments were conducted in a HEPES 2‐[4‐(2‐hydroxyethyl)piperazin‐1‐yl]ethanesulfonic acid buffer with pH 7.5 and 150 mmol L −1 of NaCl. Although poly(allylamine) is a weak cationic polymer with pK a ranging from 8.6 80 to 8.7, 81 its apparent pK a remained below pH under the experimental conditions (based on a rough estimate that 1 mmol L −1 of a monovalent salt in an aqueous solution induces reduction of pK a by 0.1) 80 . Details of the preparation of the microgel are provided in Appendix S1.…”
Section: Fitting Of Experimental Datamentioning
confidence: 99%