Chitosan-telmisartan polymeric cocrystals for improving oral absorption: In vitro and in vivo evaluation

Ganesh, Mani; Ubaidulla, Udhumansha; Rathnam, Grace; Jang, Hee-Jin

doi:10.1016/j.ijbiomac.2019.03.141

Cited by 29 publications

(14 citation statements)

References 31 publications

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“…The DSC of pure TEL shows a sharp melting endothermic peak that stretches from 261 °C to 273.75 °C, with a peak maximum at 270.5 °C (Figure ), and the enthalpy of fusion is 105.25 J/g, which is consistent with the data of Ganesh and Liu et al , The melting temperature (onset in Figure ) of SAC is 226.98 °C, which is in excellent agreement with the previous study value onset = 226.3 °C, but the enthalpy of fusion has some deviations, which may be related to the selection range of the melting peak . The endothermic peak of TEL-SAC cocrystal is extended from 211.29 to 222.38 °C, with a peak maximum at 219.98 °C; the value of the endothermic peak decreases due to the formation of TEL-SAC cocrystal.…”

Section: Results and Discussionsupporting

confidence: 91%

Solid–Liquid Phase Equilibrium and Ternary Phase Diagrams of Telmisartan-Saccharin Cocrystal in Methanol, Ethanol, and Methanol/Chloroform Mixtures at 298.15 and 313.15 K

et al. 2020

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In this work, ternary phase diagrams of telmisartan-saccharin (TEL-SAC) cocrystal in methanol, ethanol, and quasi-ternary sections of the quaternary system TEL-SAC–chloroform–methanol were determined at 298.15 and 308.15 K. The results show that the stable region of cocrystal is greatly biased towards SAC in methanol and ethanol; this is due to the large solubility difference between TEL and SAC. In the mixed solvent of chloroform and methanol, the cocrystal stable region appears at the center of the whole phase diagram when the mass fraction of chloroform is 80%, which indicated that the solubility difference between TEL and SAC in the mixed solvent was relatively small. Moreover, the solubility behavior of TEL-SAC cocrystal was studied and the results showed that the solution complexation model in methanol and ethanol was 1:1 + 1:2, and the complexation model in chloroform and binary mixtures of chloroform/methanol was 1:1.

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Section: Results and Discussionsupporting

confidence: 91%

Solid–Liquid Phase Equilibrium and Ternary Phase Diagrams of Telmisartan-Saccharin Cocrystal in Methanol, Ethanol, and Methanol/Chloroform Mixtures at 298.15 and 313.15 K

et al. 2020

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“…Accordingly, the optimized formulation fitted with all dissolution models and the values were shown in Table 6. A good correlation co-efficient (r 2 < 0.9178) was found in Higuchi kinetics, which indicates optimum dominated mechanism 10 . The release exponent of the Peppas model (n <07) indicates anomalous (non-fickian) transport and rates as a function of time follow zeroorder release.…”

Section: Mucoadhesive Study (%)mentioning

confidence: 70%

Development of Silymarin Entrapped Chitosan Phthalate Nanoparticles for Targeting Colon Cancer

Ubaidulla

Sinha

Sangavi

et al. 2022

JNR

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The present paper deals with the development of silymarin entrapped Chitosan Phthalate (CP) nanoparticles for targeting colon cancer. The QbD approach is applied to optimize the silymarin loaded chitosan phthalate nanoparticles. DOE was employed to evaluate the dependent variables from the responses of CP nanoparticles. The CP NPs were found to be 140% of mucoadhesivity at pH 7.4, superior to pH 1.2 (10%). The result revealed the chemical or ionic bond formation between the positively charged amino groups of chitosan phthalate and the negatively charged sialic acid residue of mucin present in the mucous membrane. In vitro drug release profiles were carried out under acidic and basic pH conditions. The release of encapsulated silymarin was found to be poor in acidic conditions and maximum in basic conditions. The results suggested that chitosan phthalate nanoparticles could have the potential to enhance the bioavailability of silymarin.

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“…Fig. 3 reveals that increase in the average size of these cocrystals was found to be increased with the combination of drug and CS (with increasing concentration of chitosan) [18].…”

Section: Effect Of the Process Parameters On The Loading Efficiencymentioning

confidence: 92%

Enhancement of Dissolution Rate and Bioavailability of Nifedipine by Chitosan Based Cocrystallization Technique

Reetu

Yadav²,

Singh³

et al. 2021

JPRI

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The objective of present study was to enhance solubility and dissolution behaviour of nifedipine by using cocrystallization method. A significant increase in solubility and dissolution rate of nifedipine has been demonstrated by solvent change method using chitosan. In this method, chitosan was precipitated on nifedipine crystals using sodium citrate as a salting out agent. An accurately weighed chitosan was dissolved in 1% acetic acid and drug was added in the chitosan solution. This resulting solution was added drop wise into 1% sodium citrate solution with continuous stirring. Sodium citrate precipitate polymer on drug crystals. FTIR, DSC, XRD, SEM, In-vitro dissolution studies, were studied for characterization of prepared cocrystals. Stability studies showed a good stability character of prepared cocrystals. Design Expert® software version 10.0 was used to develop polynomial models which were analysed to delineate the main effects for each CQA (critical quality attributes) through Box-Bhenken design expert. Pharmacokinetic study clearly showed the enhancement of dissolution rate of cocrystals. The above investigation concluded that the significant dose reduction is possible for nifedipine with cocrystal formulation which leads to improve patient compliance.

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Chitosan-telmisartan polymeric cocrystals for improving oral absorption: In vitro and in vivo evaluation

Cited by 29 publications

References 31 publications

Solid–Liquid Phase Equilibrium and Ternary Phase Diagrams of Telmisartan-Saccharin Cocrystal in Methanol, Ethanol, and Methanol/Chloroform Mixtures at 298.15 and 313.15 K

Solid–Liquid Phase Equilibrium and Ternary Phase Diagrams of Telmisartan-Saccharin Cocrystal in Methanol, Ethanol, and Methanol/Chloroform Mixtures at 298.15 and 313.15 K

Development of Silymarin Entrapped Chitosan Phthalate Nanoparticles for Targeting Colon Cancer

Enhancement of Dissolution Rate and Bioavailability of Nifedipine by Chitosan Based Cocrystallization Technique

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