????? Microspheres and microcapsules

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????? Microspheres and microcapsules
2
???? definitions

• ??(microspheres)??????????????????????????????????
  ??(matrix type)?????
• ??(microcapsules)????????????????????????(reservoi
  r type)?????
• ???????(microparticles)??????????,???1-300?m,?????
  800?m?

3
?????????

• 1.???
• 2.???????
• 3.????
• 4.?????
• 5.????????

4

• ???? (triptorelin)?LHRH?????, ?PLGA?????Ipsen????,
  1986???, ??? 1??, ???????????
• ????(leuprorelin)?LHRH???, ?????LHRH 15?????
  1?????????????????????,? 1 989????????
• ?????LHRH????????????,?????(buserelin)??

5

• ???????????????????,??????,??????????,
  ??????????????,??????????
• ?????, ???????????????, ????????????,?????????????
  ?????
• ????WHO????????????????????????

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????/???? Materials for encapsulation

• 1.???
• ???(core materials)?????????????????????,?????????
  ?????????????????????????????
• ????????????????

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????/???? Materials for encapsulation

• 2.?? ?????
• (1)????
• (2)????????
• (3)???????
• (4)??????,??????????
• (5)??????????
• (6)???????????????????

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????/???? Materials for encapsulation

• 3.?????
• (1)???????
• ???????????
• ?? gelatin?????1.5?2.5?????
• ???????A??? ???7-9
• ???????B? ???4.7-5
• ???????,??????
• ???20-100g/L

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????/???? Materials for encapsulation

• ????Arabica acacia
• ?????????????????????
• ????????, ??????20-100 g/L,??????????????
• ??? Chitosan
• ??????????????????????
• ?????????,??????,???????????,??????????????

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????/???? Materials for encapsulation

• ????Alginate
• ???????,???????????????????????????,??????????????
  ?,???????????
• ?????????,?????????CaCl2???????/?, ???10g/L?
• ??????,????80??30???????????????????????????

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????/???? Materials for encapsulation

• (2)????????
• ???????
• CMC-Na????????????,????????????,????1-5g/LCMC-Na?3
  0g/L??,??21???
• ????????
• ????????(CAP)???????,???pH6??????????????,???30g/L
  ,????????

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????/???? Materials for encapsulation

• ????? Ethyl cellulose
• ?????Methyl cellulose
• ??????Hydroxylmethyl cellulose

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????/???? Materials for encapsulation

• (3)???????
• ????????????(PLA)?????????????????????????????????
  ???????????????-?????????(PLA-PEG)?
  e-??????????????????????????
• ?????????????????????,??????

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??????? Preparation of microspheres

• 1. ?????
• ?????25????????,?????????????,??W/O????
• ????????100130 ºC,?????????????????,???160180
  ºC,???????????????,????20??,??????????,??????,????
  ??

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??????? Preparation of microspheres

• 2. ???????
• ????????????????,???????????,????????????
• ? ???????
• ????????04ºC???????????(pH 7.5),????????????,????
  ??,??,???????????????????,????,???Span80????????,
  ????,??????????

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??????? Preparation of microspheres

• 3. ?????
• ??????????????????????????????

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? ?????PLA?????????
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??????? Preparations of microcapsules

• ?????????????????
• (?)?????
• ???????????,??????????????????,??????????(ph
  ase separation coacervation)?????????????4?
• ??????
• ?????
• ?????
• ?????

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??????? Preparations of microcapsules

• 1.????
• ????(simple coacervation)?????????????,????????(??
  ?)?????????????????????????????
• ????????????????,???????(???????????????,????),??
  ?????????????????,?????????,???????,??????????????
  ?

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??????? Preparations of microcapsules

• 2.????
• ????(complex coacervation)???????????????????????,
  ?????????????????????
• ????????????????(?CMC?CAP???)?????????????????????
  ???????

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??????? Preparations of microcapsules

• ???????????????????,??????pH????????????(pH4.0-4.
  5),?????????,????????,?????????????,???????????
• ?????????????,??????????,?????????????

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? ??????????????????????????(?????1µm)? A,?FITC(f
luorescein isothiocyanate)????????????????????????
??????????? B,???????RBITC(rhodamine B
isothiocyanate)?????????????????
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? ????FITC?????RBITC??????????????????????????(??
???1µm)?
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• 3.?? ????
• ?? ????(solvent-nonsolvent)??????????????????(??
  ?),?????,????????????
• ????????????????/????/?????
• ??????????,??????????????,??????

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• 4.?????
• ???????,??????????EC????,????????,??????
• ?????(PIB)??????????????
• ???????PIB/EC/?????????,?80????????,????45?,?????
  25?,EC??????

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• 5.?????
• ???????????????????????????????(in-liquid
  drying),?????????
• ????????????????????????(?????)????????

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??????? Preparations of microcapsules

• (?)?????
• 1.????? spray drying
• ???????????????,??????????????,?????????(????????
  ),?????????????????,???????
• ????????????????????????????????????????????????

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• 2.?????
• ?????????????,?????????????,???????(spray
  congealing)?
• ??????????????????,??????????,??????????

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• 3.?????
• ?????(air suspension)????????,???????????????????,
  ????????????????,???????????????,?????????????????
  
• ???????????,35-5000micron?
• ????????,??,??,?,????????????????????????????????

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??????? Preparations of microcapsules

• (?)???
• ???????????????????????,????,????,??????????????
• ??????????,?????W/O????,????????????
• 1.?????
• ?????(interface polycondensation),?????(??)????(??
  ?)??????????????

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• 2.?????
• ???????????,?Co60????????,???????????
• ???????,????????????

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?????????? Characterization

• 1.????????
• 2.????/??????
• 3.??/?????????
• 4.????/??????????
• 5. ????????????????

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????????

1. ??????????????
2. ?????????????
3. ??????????????