The aims of this study were to prepare and characterize hydroxypropyl methylcellulose(HPMC)/polycarbophil(PC) mucoadhesive blend films saturated with propranolol hydrochloride(PNL)-loaded nanoparticles to improve perm...The aims of this study were to prepare and characterize hydroxypropyl methylcellulose(HPMC)/polycarbophil(PC) mucoadhesive blend films saturated with propranolol hydrochloride(PNL)-loaded nanoparticles to improve permeability of drugs that undergo firstpass metabolism. An ionic cross-linking method and film casting technique was used to prepare nanoparticles and mucoadhesive blend films, respectively. Increasing concentrations of PNL(70, 80, 90 mg/film) in HPMC/PC blend films containing PNL-loaded nanoparticles(PN-films) and HPMC/PC blend films containing PNL(80 mg/film) without nanoparticles(PPfilms) were prepared to test swelling, mucoadhesiveness, release, permeation and physicochemical properties. Scanning electron microscope(SEM) images showed a partially smooth surface with a wrinkled occurrence and spherically shaped, well-dispersed nanoparticles on the surface of PN-films containing PNL 80 mg/film(PN-films-80). The size of the nanoparticles on the surface of PN-films-80 was around 100 nm, which was similar to the nanoparticle size observed using light scattering technique. The swelling index(SI)of all PN-films and PP-films increased greatly in the first period time(10–20 min) and reached swelling equilibrium at 20 min and 30 min, respectively. For the PN-films, the concentration of PNL influenced the mucoadhesive properties and tended to be higher when the amount of PNL increased. Immediate release of all blend film formulations was found in early time points(10–30 min). After 120 min, the release of PN-films-70 was lower than the other PNfilms. Permeation studies using porcine buccal mucosa showed that inclusion of nanoparticles in the films increased the permeability of PNL compared to PP-films. Therefore, buccal administration of mucoadhesive blend films containing PNL-loaded nanoparticles could be a promising approach for drugs that undergo first-pass metabolism.展开更多
Polycarbophil(PCP),a kind of pharmaceutical polymers with superior bioadhesive properties has been widely used in the field of controlled drug delivery systems.It could be used as a highly efficient thickener,bioadhe...Polycarbophil(PCP),a kind of pharmaceutical polymers with superior bioadhesive properties has been widely used in the field of controlled drug delivery systems.It could be used as a highly efficient thickener,bioadhesive agent,suspending aid and emulsion stabilizer when dispersed in water or other polar solvents.These exceptional utilities of the polymers result from their hydrophilic nature.Hydrogen bonding plays an important role in most adhesion behaviours and becomes the main adhesion force.This paper reviews the applications of PCP in pharmacy over the past decades,and clarifies its unique advantages in the bioadhesive formulations.After an introduction discussing its structural characteristics and action mechanism,the focus turned to the description of its available applications in detail with particular emphasis on the ocular,nasal,vagina and oral drug delivery systems.The other less developed formulations are also described,including the buccal and the transdermal delivery systems.展开更多
基金the financial support provided by Thammasat University under the TU Research Scholar,Contract No.TP 2/68/2556
文摘The aims of this study were to prepare and characterize hydroxypropyl methylcellulose(HPMC)/polycarbophil(PC) mucoadhesive blend films saturated with propranolol hydrochloride(PNL)-loaded nanoparticles to improve permeability of drugs that undergo firstpass metabolism. An ionic cross-linking method and film casting technique was used to prepare nanoparticles and mucoadhesive blend films, respectively. Increasing concentrations of PNL(70, 80, 90 mg/film) in HPMC/PC blend films containing PNL-loaded nanoparticles(PN-films) and HPMC/PC blend films containing PNL(80 mg/film) without nanoparticles(PPfilms) were prepared to test swelling, mucoadhesiveness, release, permeation and physicochemical properties. Scanning electron microscope(SEM) images showed a partially smooth surface with a wrinkled occurrence and spherically shaped, well-dispersed nanoparticles on the surface of PN-films containing PNL 80 mg/film(PN-films-80). The size of the nanoparticles on the surface of PN-films-80 was around 100 nm, which was similar to the nanoparticle size observed using light scattering technique. The swelling index(SI)of all PN-films and PP-films increased greatly in the first period time(10–20 min) and reached swelling equilibrium at 20 min and 30 min, respectively. For the PN-films, the concentration of PNL influenced the mucoadhesive properties and tended to be higher when the amount of PNL increased. Immediate release of all blend film formulations was found in early time points(10–30 min). After 120 min, the release of PN-films-70 was lower than the other PNfilms. Permeation studies using porcine buccal mucosa showed that inclusion of nanoparticles in the films increased the permeability of PNL compared to PP-films. Therefore, buccal administration of mucoadhesive blend films containing PNL-loaded nanoparticles could be a promising approach for drugs that undergo first-pass metabolism.
基金the work was supported by a research group from Shenyang Pharmaceutical University,including the financial support.And get the vigorous help from all the teachers and students of Pharmacy Department.
文摘Polycarbophil(PCP),a kind of pharmaceutical polymers with superior bioadhesive properties has been widely used in the field of controlled drug delivery systems.It could be used as a highly efficient thickener,bioadhesive agent,suspending aid and emulsion stabilizer when dispersed in water or other polar solvents.These exceptional utilities of the polymers result from their hydrophilic nature.Hydrogen bonding plays an important role in most adhesion behaviours and becomes the main adhesion force.This paper reviews the applications of PCP in pharmacy over the past decades,and clarifies its unique advantages in the bioadhesive formulations.After an introduction discussing its structural characteristics and action mechanism,the focus turned to the description of its available applications in detail with particular emphasis on the ocular,nasal,vagina and oral drug delivery systems.The other less developed formulations are also described,including the buccal and the transdermal delivery systems.
