Formulation and release of alaptide from cellulose-based hydrogels

Abstract

The modern drug alaptide, synthetic dipeptide, shows regenerative effects and effects on the epitelisation process. A commercial product consisting of 1% alaptide hydrophilic cream is authorised for use in veterinary practice. This study focuses on the formulation of alaptide into semi-synthetic polymer-based hydrogels. The aim of the present study is to prepare hydrogels and to evaluate the liberation of alaptide from hydrogels. The hydrogels were prepared on the basis of three gel-producing substances: methylcellulose, hydroxyethylcellulose and hydroxypropylcellulose. To enhance the drug release from hydrogel humectants, glycerol, propylene glycol and ethanol in various concentrations were evaluated. The permeation of the alaptide from gels into the acceptor solution was evaluated with the use of the permeable membrane neprophane. The amount of drug released from prepared hydrogels was determined spectrophotometrically. Hydrogels with optimal alaptide liberation properties were subjected to the study of rheological properties in the next phase. The optimal composition of hydrogel as established in this study was 1% alaptide + 3% hydroxyethylcellulose with the addition of 10% glycerol as humectant. Due to the advantageous properties of hydrogels in wounds, alaptide could be incorporated into a hydrogel base for use in veterinary medicine. , gel-producing substance, humectant, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose Hydrogel research increased significantly in the last decades; due to their properties, hydrogels are widely used as suitable bases of preparations in human and veterinary medicine. The properties of hydrophilic gels, or hydrogels, are significantly different from those of ointments and creams. Hydrogels are usually formed by hydrophilic polymers which under certain conditions and polymer concentrations create a gel with a high percentage of water. They can additionally contain glycerol or propylene glycol as humectants and ethanol as an antimicrobial agent. Hydrogels create a smooth film that adheres well, can be removed easily and exhibits a cooling effect. The active substances have been dispersed in hydrogels (dissolved, suspended or emulsified). The base with the incorporated active ingredient must have suitable properties, especially biocompatibility and chemical, microbiological and physical stability (Bronaugh and Maibach 2001). EpitelisationPeptide drugs are becoming an essential part of modern therapy. Beside their therapeutic effect they can perform the function of another non-peptide drug carrier. Their reactions on changes of the pH milieu, biocompatibility, thermosensitivity and good mechanical properties have been reported (Galaev and Mattiasson 2008).Alaptide is spirocyclic synthetic dipeptide, chemically prolyl-leucyl-glycine amide derivative (Nedvidková et al. 1994). Due to its positive influence on regenerative processes in various skin diseases it can be used in veterinary medicine. For a long time it has been used as a commercial 1% hydrophilic ...

Cellulose-based hydrogel materials: chemistry, properties and their prospective applications

“…Controlled release of other proteins including dextran, ketoprofen, bovine serum albumin (BSA) and alaptide have been reported by some studies through the development of IPN and semi-IPN HPC-PAA, polyacrylamide-grafted-xanthan (PAAm-g-XG) and other CB hydrogels (methylcellulose, hydroxyethyl cellulose and hydroxypropyl cellulose), respectively (Chen and Fan 2008 ; Kulkarni and Sa 2008 ; Sklenář et al 2013 ; Xu et al 2010 ). Dutta et al ( 2016 ) have prepared two types of triple (pH, temperature and redox) stimuli responsive hydrogels from carboxymethyl cellulose (CMC) and poly( N -isopropylacrylamide), where one is prepared by copolymerization (copolymerizing N -isopropylacrylamide) and the other one, methacrylated carboxymethyl cellulose, is by polymerizing NIPA in the presence of CMC.…”

Preparation and Characterization of Alginate and Chitosan Ipc Based Gel Formulation for Mucosal Application

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Association, Distribution, Liberation, and Rheological Balances of Alkyldimethylbenzylammonium Chlorides (C12–C16)

“…Therefore, the obtained results will be used in ongoing research activities at the workplace of the authors. The aim of this research is to develop optimal control of drug liberation from semisolid dosage forms and computer simulation of the LADME process with possible prediction of the therapeutic effect [ 1 , 18 , 19 , 20 ].…”