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. Author manuscript; available in PMC: 2023 Oct 1.
Published in final edited form as: Pharmacol Ther. 2022 Mar 26;238:108177. doi: 10.1016/j.pharmthera.2022.108177

Table 2:

Drug release and biodistribution properties of capsaicin sustained release drugs

Name of drug Type of sustained release formulation Composition of sustained release formulation In Vitro drug release In vivo biodistribution studies
Drug release pattern Cellular uptake of drug Comparison of drug release pattern with free capsaicin/blank formulation Models Organ biodistribution Comparison of drug release pattern with free capsaicin/ blank formulation
CAP-UREA-SDDDS Solid State dispersion system Urea scaffold
  • Approximately 38% of the drug cargo (capsaicin) was released within the first hour

  • Approximately 100% of the capsaicin was released within 8 days

ND CAP-UREA-SDDS released capsaicin more slowly than free capsaicin ND ND ND
CAP-SOY-PL




Phospholipid complexes Soyabean phospholipids
  • Approximately 60% of the capsaicin was released within 10 hours

  • Approximately 100% of the drug was released at 30 hours

ND CAP-SOY-PL released capsaicin more slowly than free capsaicin ND ND ND
CAP-CUR-GLY-GAL-LIPO
Liposome
DSPE-PEG
  • Approximately 60% of the drug

  • cargo (capsaicin) was released within 15 hours

  • Approximately 60% of the drug

  • 95% of the drug was released at 48 hours

  • Maximal uptake of liposomal drugs is at 4 hours in HepG2 cells

  • At 4 hours the uptake of GLY-GAL-LIPO> GLY-LIPO=GAL-LIPO>blank-LIPO

  • Maximal retention of liposomal drugs is at 12hours hours in HepG2 /LX2 co-cultured cells

  • At 12 hours and 24 hours the retention of GLY-GAL-LIPO> GLY-LIPO=GAL-LIPO>blank-LIPO

  • Drug retention of GLY-, GAL-functionalized liposomes was greater than free capsaicin

B16/H22 tumor-bearing Balb/c mice
  • Most of the GLY-, GAL-functionalized liposomes were found in the liver.

  • GLY-, GAL-functionalized liposomes were only localized to the H22 liver tumor. No liposomes were detected in the B16 melanoma tumor

  • GLY-, GAL-functionalized liposomes showed deep penetration inside the solid H22 liver tumor

ND