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(3) ¿¼²ì²»Í¬PHÖµ£¨PH=4.3¡¢PH=5.6ºÍPH=7.4£©¡¢²»Í¬ÔØÒ©ÂÊ£¨9.53%¡¢17.48%ºÍ26.37%£©ÒÔ¼°Å¼ÁªÅäÌå¶ÔÄÉÃ×Á£ÊÍÒ©ÐÔÄܵÄÓ°Ï죬²¢Ä£ÄâÈËÌåÄÚ²¿»·¾³½øÐÐÊÍÒ©ÐÐΪµÄÑо¿£¬·ÖÎöÿ¸ö½×¶ÎµÄÊÍÒ©»úÀí£¬ÄâºÏÎåÖÖ³£¼ûÒ©ÎïÄ£Ð͵ÄÇúÏß·½³Ì²¢Ñ¡Ôñ×î¼ÑÊÍÒ©Ä£ÐÍ¡£
(3) the influence of pH values (pH = 4.3, 5.6 and 7.4), drug loading rates (9.53%, 17.48%, and 26.37%), and the of coupling ligands on the drug release properties of nanoparticles were studied, and the internal environment release behavior of body was simulated, the release mechanism in different stage was analysed, the best drug delivery model was selected through fitting the curve equation model of five kinds of common drugs.
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Results: (1) the best fabrication process of three kinds of drug-loaded nanoparticles were determined through the investigation of single factor and orthogonal design, drug loading rates of the three kinds of drug-loaded nanoparticles obtained in the optimal preparation process were 26.9%, 27.4%, and 30.3%, respectively, while the encapsulation efficiency of that were 66.5%, 67.2%, and 73.6%. The average diameter of obtained nanoparticles were 110nm, 117nm, and 125 nm, respectively, with smooth and rounded morphology, good dispersion, and narrow particle size distribution.
(2) ÓúìÍâ¹âÆ×£¨IR£©±íÕ÷ÄÉÃ×Á£±íÃæ·Ö×Ó»ùÍŵı仯£¬±íÃ÷FAºÍHA·Ö±ðͨ¹ýõ£°·¼ü×÷Óóɹ¦µÄżÁªµ½ÁËÄÉÃ×Á£±íÃ档ȷ¶¨ÁËFAºÍHAµÄ×î¼ÑżÁª¹¤ÒÕ£¬ÔÚ×î¼ÑżÁª·´Ó¦Ìõ¼þÏÂFAºÍHAµÄżÁªÁ¿·Ö±ðΪ0.0237¡Á10-3mol/gºÍ0.0178¡Á10-6mol/g¡£Á£¾¶·ÖÎö±íÃ÷FAżÁªÇ°ºóÄÉÃ×Á£Á£¾¶»ù±¾Îޱ仯£¬HA£¨Mr=300000£©Å¼ÁªºóÁ£¾¶ÓÉ122.2nmÔö³¤µ½131.3nm£¬±íÃ÷´ó·Ö×ÓÁ¿µÄHA¶ÔÁ£¾¶±ä»¯Ó°Ïì½Ï´ó¡£Í¨¹ý·Å´ó²»Í¬±¶ÊýµÄSEMÕÕƬ¿É¿´³öÅäÌåżÁªºóÄÉÃ×Á£·Ö²¼¾ùÔÈ£¬·ÖÉ¢ÐԽϺã»
The change of molecular groups on nanoparticle surface were characterized by infrared spectroscopy (IR), the study results indicated that HA and FA groups were successfully coupled to the nanoparticles with the amide bonds. The coupling amount of FA and HA under the optimal process, which was decided in our experiment, were 0.0237 ¡Á 10-3mol/g and 0.0178 ¡Á 10 6 mol/g. The results of particle size analysis showed that the size of nanoparticles were same before and after the FA coupling, while the particles size increased from 122.2nm to 131.3nm with the HA(Mr=300000) coupling, which indicated that the high molecular weight HA has a great impact on particle size. The SEM photographs with different magnification showed the uniform distribution and good dispersion of ligand coupled nanoparticle
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Drug release rate and the cumulative amount of drug release of nanoparticles decreased with the increasing pH values(4.3, 5.6, and 7.4), and the stronger acidity within a certain pH range leads to a higher release rate and cumulative release, release rate of high drug loading nanoparticles is higher than that in middle and low drug loading nanoparticles in the same conditions, the influence of FA coupling on the drug release properties of nanoparticles was little, drug release rate was significantly reduced after macromolecular HA coupled to the surface of the nanoparticles. targeting PLA drug-loaded nanoparticles exhibited good controlled-release effect in simulated environment of body, the fitted FA and HA-PLA drug release model of the drug-loaded nanoparticles were ININ (1 / (1-Q)) = 0.04633 Int-1.03562 and 1-Q1 / 3 =-0.01368t +1.04726, respectively. |
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