Abstract:Temperature is a widely incorporated stimulus in pharmaceutical applications because of its efficiency as a therapeutic medium; thus, substantial evidence on temperature‐responsive polymer applications is reported. Poly(N‐isopropylacrylamide) (PNIPAAm) is a well‐established, temperature‐responsive polymer that exhibits a low critical solution temperature (LCST) at ≈ 32°C, which is close to physiological temperature. Hence, they are widely used in various pharmaceutical applications, such as drug delivery with … Show more
“…Furthermore, the ability to alter the physicochemical characteristics of PNIPAM through copolymerization provides a great scope for modifying the base polymer as per the required application. 19,20 In this work, we have developed a sprayable thermoresponsive (PNIPAM-based) formulation that upon administration inside the colon can instantly form a physical coating onto the colon wall to timely cover the wound openings, prevent bacterial translocation, provide optimum drug concentration at the diseased site, and promote mucosal self-repair and regeneration. To achieve such outcomes using our therapeutic formulation, we have incorporated hyaluronic acid into the PNIPAM chains.…”
Section: Introductionmentioning
confidence: 99%
“…Poly( N -isopropylacrylamide) (PNIPAM) has been one of the most studied thermoresponsive polymers due to the ease of polymer synthesis and its physiological lower critical solution temperature (∼32 °C) in water. Furthermore, the ability to alter the physicochemical characteristics of PNIPAM through copolymerization provides a great scope for modifying the base polymer as per the required application. , …”
Impairment of intestinal epithelium is a typical feature of inflammatory bowel disease (IBD) that causes leakage of bacteria and antigens from the intestinal lumen and thus results in persistent immune activation. Hence, healing and regeneration of the damaged gut mucosa is a promising therapeutic approach to achieve deep remission in IBD. Currently, available systemic therapies have moderate effects and are often associated with numerous side effects and malignancies. In this study, we aimed to develop a topical therapy by chemically conjugating a temperature-responsive polymer, i.e., poly(N-isopropylacrylamide), along with hyaluronic acid to obtain a sprayable therapeutic formulation that upon colon instillation adheres to the damaged gut mucosa due to its temperature-induced phase transition and mucoadhesive properties. An ex vivo adhesion experiment demonstrates that this therapeutic formulation forms a thin physical coating on the mucosal lining at a physiological temperature within 5 min. Physicochemical characterization of (P(NIPAM-co-NTBAM)-HA) established this formulation to be biocompatible, hemocompatible, and non-immunogenic. Prednisolone was encapsulated within the polymer formulation to achieve maximum therapeutic efficacy in the case of IBD-like conditions as assessed in a custom-fabricated perfusion-based ex vivo model system. Histological analysis suggests that the prednisolone-encapsulated polymer formulation nearly restored the mucosal architecture after 2,4,6trinitrobenzenesulfonic acid-induced damage. Furthermore, a significant (p ≤ 0.001) increase in mRNA levels of Muc-2 and ZO-1 in treated groups further confirmed the mucosal epithelial barrier restoration.
“…Furthermore, the ability to alter the physicochemical characteristics of PNIPAM through copolymerization provides a great scope for modifying the base polymer as per the required application. 19,20 In this work, we have developed a sprayable thermoresponsive (PNIPAM-based) formulation that upon administration inside the colon can instantly form a physical coating onto the colon wall to timely cover the wound openings, prevent bacterial translocation, provide optimum drug concentration at the diseased site, and promote mucosal self-repair and regeneration. To achieve such outcomes using our therapeutic formulation, we have incorporated hyaluronic acid into the PNIPAM chains.…”
Section: Introductionmentioning
confidence: 99%
“…Poly( N -isopropylacrylamide) (PNIPAM) has been one of the most studied thermoresponsive polymers due to the ease of polymer synthesis and its physiological lower critical solution temperature (∼32 °C) in water. Furthermore, the ability to alter the physicochemical characteristics of PNIPAM through copolymerization provides a great scope for modifying the base polymer as per the required application. , …”
Impairment of intestinal epithelium is a typical feature of inflammatory bowel disease (IBD) that causes leakage of bacteria and antigens from the intestinal lumen and thus results in persistent immune activation. Hence, healing and regeneration of the damaged gut mucosa is a promising therapeutic approach to achieve deep remission in IBD. Currently, available systemic therapies have moderate effects and are often associated with numerous side effects and malignancies. In this study, we aimed to develop a topical therapy by chemically conjugating a temperature-responsive polymer, i.e., poly(N-isopropylacrylamide), along with hyaluronic acid to obtain a sprayable therapeutic formulation that upon colon instillation adheres to the damaged gut mucosa due to its temperature-induced phase transition and mucoadhesive properties. An ex vivo adhesion experiment demonstrates that this therapeutic formulation forms a thin physical coating on the mucosal lining at a physiological temperature within 5 min. Physicochemical characterization of (P(NIPAM-co-NTBAM)-HA) established this formulation to be biocompatible, hemocompatible, and non-immunogenic. Prednisolone was encapsulated within the polymer formulation to achieve maximum therapeutic efficacy in the case of IBD-like conditions as assessed in a custom-fabricated perfusion-based ex vivo model system. Histological analysis suggests that the prednisolone-encapsulated polymer formulation nearly restored the mucosal architecture after 2,4,6trinitrobenzenesulfonic acid-induced damage. Furthermore, a significant (p ≤ 0.001) increase in mRNA levels of Muc-2 and ZO-1 in treated groups further confirmed the mucosal epithelial barrier restoration.
“…4,5 For example, temperature-responsive polymers, which have received more attention from researchers, show a phase transition at a specific temperature, resulting in a sudden change in the dissolved state. 6–13 The best known temperature-responsive polymer is poly( N -isopropylacrylamide) (PNIPAM), which has a lower critical solution temperature (LCST) and has become a major material in the versatile and dynamic area of polymer science. 8,9 Polymers with ionizable groups such as the amine group, the carboxyl group, etc ., whose degree of ionization varies with pH, often exhibit pH-response.…”
Section: Introductionmentioning
confidence: 99%
“…6–13 The best known temperature-responsive polymer is poly( N -isopropylacrylamide) (PNIPAM), which has a lower critical solution temperature (LCST) and has become a major material in the versatile and dynamic area of polymer science. 8,9 Polymers with ionizable groups such as the amine group, the carboxyl group, etc ., whose degree of ionization varies with pH, often exhibit pH-response. 14–18 There are many pH changes in biological systems; especially when the tissue is diseased, the pH will be mutated, so in the field of biological medicine, pH-responsive polymers as intelligent targeted drug carriers have broad application prospects.…”
Novel temperature/pH/CO2-triple responsive homopolymers bearing different end substituents which showing different responsive properties, and they have good application prospects in self-assembly, biomedicine and other fields.
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