Abstract
Objective: Thiomers have been known as polymer with mucoadhesive properties. The aim of this study was to synthesize the mucoadhesive potential of hydroxypropyl cellulose-cysteamine conjugate (HPC-cysteamine).Methods: The parent polymer HPC was chemically modified by introducing sulphydryl bearing compound using reductive amination. HPC-cysteamine conjugates were prepared at reaction pH value of 5. The reaction was stabilized by the addition of cyanoborohydride. Afterwards, the conjugate was evaluated for optimum free thiol group, swelling behavior, viscosity and mucoadhesive properties.Results: The conjugates showed maximum thiol incorporation on HPC of 1063.03±64.27 µmol/g. The disulphide groups content was 278.71±32.14 μmol/g. Mucoadhesion studies revealed that mucoadhesion of HPC-cysteamine demonstrated 26 h. The swelling behaviour of HPC-cysteamine tablets increased within the time period of study. The viscosity of HPC-cysteamine was higher than that of unmodified HPC. The thermal profile of HPC-cysteamine and unmodified HPC analyzed by differential scanning calorimetry (DSC) displayed a different enthalpy (ΔH) value.Conclusion: HPC-cysteamine conjugate renders better properties which might be more beneficial for drug delivery system compared to unmodified HPC.
Highlights
The development of multifunctional polymers in pharmaceutical technology has been influenced by various factors, including biocompatible and biodegradable properties
Thiomers are polymers modified by introducing thiol groups on the structure of the polymer backbone by chemical reactions
Unmodified hydroxypropyl cellulose (HPC) was reacted with sodium periodate to obtain oxidized HPC
Summary
The development of multifunctional polymers in pharmaceutical technology has been influenced by various factors, including biocompatible and biodegradable properties. Thiomers are polymers modified by introducing thiol groups on the structure of the polymer backbone by chemical reactions. They are preferred for improving bioavailability of drugs and a fascinating choice for oral drug delivery. The administration of macromolecule drugs such as protein drugs is required in several diseases Their effectiveness is still poor due to low bioavailability the application of thiolated polymers might be beneficial to overcome the problems in their delivery. These multifunctional polymers demonstrate some advantages in mucoadhesion and permeation enhancing properties compared to unmodified polymers [3, 4]
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