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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 6:

Drug Release and biodistribution Properties of capsaicin nanoparticle drugs

Name of nanoparticle drug Type of nanoparticle Composition of nanoparticle In Vitro drug release In vivo biodistribution studies
Drug release pattern Comparison of drug release pattern with free capsaicin/blank nanoparticles Models Organ biodistribution Comparison of drug release pattern with free capsaicin/ blank nanoparticles
CND Dendrimers Oleoyl chloride bound to PEG 400 ND ND ND ND ND
CAP-HAP-PXS-NPs Nanocomposite polymers PXS polymers wrapped around HAP nanorods

  • Less than 10% of the drug cargo (capsaicin) was released within 24hours

  • Approximately 60% of the drug was released at 10 days

 ND ND ND ND
CAP-SNEDDS Self-assembling nanoemulsifying drug delivery systems Isopropyl myristate, Tween-80 and ethanol

  • Approximately 80% of the drug cargo (capsaicin) was released within 15 minutes

  • Approximately 100% of the drug was released at 45 minutes and maintained at 100% till 90 minutes

  • CAP-SNEDDS released capsaicin more slowly than free capsaicin

 Wistar Albino rats ND

  • CAP-SNEDDS released capsaicin (in the plasma) more slowly than free capsaicin

  • Approximately 50% of total capsaicin released from CAP-SNEDDS was detected at 24 hours. The amounts of free capsaicin in the plasma after 24 hours were negligible

  • Bioavailability, elimination half-life, MRT of CAP-SNEDDS > free capsaicin
CAP-TMC-NP Polymeric nanoparticles Trimethyl chitosan ND ND ND ND ND
CAP-EW-MAGNETIC-NP Magnetic nanocomposite polymers Egg white coated cobalt-ferric oxide functioned zeolite hybrid

  • Approximately 65% of the drug cargo (capsaicin) was released within 24 hours

  • Greater than 70% of the drug was released between 1–5 days

  • The rate of capsaicin released from CAP-EW-MAGNETIC-NP was greater at pH=5.5 (pH of duodenum) than at pH =7.4 (pH of small intestine)

 ND ND ND ND
NIR-CAP-Gold-NR-MSN-NP Nanodots Gold nanorods embedded in mesoporous silica nanoparticles ND ND ND ND ND
CAP-mPEG-PCL Polymeric nanoparticles mPEG-PCL block copolymer

  • Greater than 80% of the drug cargo (capsaicin) was released within 24 hours

 ND C57BL6 syngeneic models of glioma

  • Capsaicin was detected in the brain

  • Peak levels of capsaicin in the brain was observed from 3 hours to 24hours

 ND
CAP-SLN Solid lipid nanoparticle Stearic acid nano-emulsion with Tween-80 as the surfactant and sodium deoxycholate as co-surfactant

  • Release of capsaicin from CAP-SLNs was maximal at pH=5.4 (pH of duodenum),

  • Maximal release of capsaicin (from CAP-SLNs) occurred at 31 hours

  • Approximately 77% of the capsaicin was released from CAP-SLNs at a pH=5.4; and 52% of the drug was released at pH=7.2 (pH of small intestine)

 ND Rattus novegicus rats

  • Maximal bioavailability of capsaicin (released from CAP-SLNs) was observed at 24 hours

  • Amount of capsaicin detected in the liver>kidney>heart> spleen>lungs

 ND
CAP-NLIPO Nanoliposome Ratio of DPPC: Cholesterol: DSPE/PEG2000 =75:20:5

  • Capsaicin was released from the nanoliposomes in a biphasic pattern at pH=7.4.

  • Initially the drug was released at a fast pace; about 12% of the capsaicin was released within the first hour

  • After 5 hours, the rate of drug release becomes slower and prolonged. About 24% of the capsaicin was released at 48 hours

  • Below 40 hours, the release of the drug (capsaicin) cargo from CAP-NLIPO was slower than free capsaicin

  • After 40 hours, the rate of drug release from CAP-NLIPO becomes slower than free capsaicin

 ND ND ND
CFLN Polymeric nanoparticles DSPE-PEG

  • Approximately 30% of the drug cargo (capsaicin) was released within 24 hours

  • The presence of FA did not have any effect on the in vitro drug release pattern

  • Both CLFN and CLN had similar in vitro drug release pattern

 Sprague Dawley Rats ND

  • Bioavailability, elimination half-life, of CFLN (in plasma) > free capsaicin
CAP-FA-PLGA-PEG-NP Polymeric nanoparticles PEG and Polylactide decoglycolic acid

  • Capsaicin was released in a biphasic pattern.

  • Initially the drug was released at a fast pace; about 35% of the capsaicin was released within the first 4 hours

  • After 4 hours, the rate of drug release becomes slower and prolonged. About 60% of the capsaicin was released at 24 hours

  • The uptake of CAP-FA-PLGA-PEG-NP > free Capsaicin in human A549 cells.

 Wistar Albino rats bearing lung tumors

  • CAP-FA-PLGA-PEG-NP

    Amount of capsaicin detected in the lung > liver > heart > spleen> kidney

  • Free Capsaicin

    Amount of capsaicin detected in the liver > spleen > kidney > heart > lung

 ND
CAP-BT-PNPP Polymeric nanoparticles PEG and polylactide decoglycolide

  • The drug cargo was released steadily within the first 5 hours, followed by a period of sluggish release, attaining the maximal levels at the end of 1 week

  • Approximately 20% of the drug cargo was released within 24 hours

  • Approximately 45–55% of the drug cargo was released at the end of 1 week

  • The presence of biotin increased the magnitude of drug released in vitro

  • The in vitro drug release efficacy of CAP-BT-PNPP > BT-NP~CAP-NP> free capsaicin

 ND ND ND
HA-PCL-CAP-NP Polymeric nanoparticles Poly ԑ-caprolactone

  • Biphasic release pattern

  • The presence of HA did not have any effect on the in vitro drug release pattern

  • The in vitro drug release efficacy of HA-PCL-CAP-NP> CAP-PCL-NP

 Wistar Albino rats bearing lung tumors HA-PCL-CAP-NP:

  • Amount of capsaicin was detected in the lung > liver > heart > spleen> kidney

CAP-PCL-NP:

  • Amount of capsaicin was detected in the liver > lung > spleen > heart > kidney

Free Capsaicin

  • Amount of capsaicin was detected in the liver > spleen >heart > kidney> lung

 Bioavailability, elimination half-life, of HA-PCL-CAP-NP (in plasma) > CAP-PCL-NP > free capsaicin
CAP-Chi-NCAS Polymeric nanoparticles Chitosan

  • CAP-Chi-NC release 3-fold higher amounts of capsaicin in T24 bladder cancer cells relative to UROtsa normal urothelial cells

 ND ND ND ND
CAP-CS-NP Polymeric nanoparticles Chitosan ND ND ND ND ND
MUC1-Apt-HSA-CAP-NP Polymeric nanoparticles Human serum albumin ND ND ND ND ND
1-SEDDS Self-emulsifying hydrophobic nanoparticle drug delivery system Tween-80

  • About 80% of the drugs from 1-SEDDS is released at 6 hours at a pH=7.4 (pH of small intestine)

  • No drug release was observed at acidic pH, specifically at pH=1.2 (pH of the stomach) or at pH=4.5, 5.4 (pH of the duodenum)

 ND ND ND 1-SEDDS does not induce hemolysis
PTX-CAP-Fmoc-PEG-NM Polymeric micelles Polyethylene glycol

  • About 30% of the drug cargo (paclitaxel) was released within 24 hours

  • About 20% of the capsaicin was released at 24 hours

  • The in vitro drug release efficacy of PTX-CAP-Fmoc-PEG-NM > free paclitaxel

  • The in vitro drug release efficacy of PTX-CAP-Fmoc-PEG-NM > free capsaicin

 Balb/c mice implanted with subcutaneous 4T1 murine breast cancer tumors

  • Amount of paclitaxel present in the tumors of PTX-CAP-Fmoc-PEG-NM-treated mice > amount of paclitaxel present in the tumors of mice administered with free paclitaxel

  • Amount of paclitaxel present in the heart, kidney of PTX-CAP-Fmoc-PEG-NM-treated tumor-bearing mice > amount of paclitaxel present in the heart, kidney of tumor-bearing mice administered with free paclitaxel

  • PTX-CAP-Fmoc-PEG-NM released paclitaxel (in the plasma) more slowly than free paclitaxel

  • Bioavailability, biological half-life of PTX-CAP-Fmoc-PEG-NM > Free paclitaxel

  • Clearance time of free paclitaxel > PTX-CAP-Fmoc-PEG-NM