Extraction, characterization and controlled release application of pectin-like/chitosan hydrogels system loaded Ciprofloxacin.

INTRODUCTION: In recent decades, drug delivery applications have extensively utilized hydrogel systems based on natural polymers. Among the numerous biopolymer-based hydrogel drug delivery systems reported, a novel pectin-like substance was extracted from fig leaves and copolymerized with chitosan. METHOD: The hydrogel was reformed into microspheres using glutaraldehyde (chemical cross-linker) and sodium hexametaphosphate (physical cross-linker). The extracted polysaccharide and the prepared hydrogels were characterized by FTIR, GC/MS, SEC/MALS/DRI as well as XRD, SEM, BET, and thermal analysis. SEM images revealed the formation of porous microspheres with an average size of 50 µm in diameter. Degrees of swelling in pH7 at 35°C have shown the hydrogels reached two to three times their weights. This has been reflected in their ability to load drugs or any other chemicals. The loading formula shows that hydrogels have maximum loading efficiency more than one-third of the weight of hydrogel. The antimicrobial ciprofloxacin was used as a model for loading on prepared hydrogels. The loaded hydrogels were tested for their biological activities against staphylococcus aureus (S. aureus) bacteria. The antimicrobial growth inhibition zone of the cultured (S. aureus) by ciprofloxacin-loaded hydrogel was followed, which shows controlled growth in inhibition zone sizes and for long time intervals. Results showed that the pectin-chitosan hydrogels exhibited significant antibacterial activity against gram - positive bacteria (S. aureus), with an inhibition zone of 45 mm for (CH-co-FLP)/GLU hydrogel. RESULT: In vitro, the ciprofloxacin-loaded hydrogels were studied and the cumulative release of ciprofloxacin under suitable conditions was found in a controlled manner and kept release for a long time interval. Data exhibited that the cumulative release profile of ciprofloxacin from the hydrogel demonstrated sustained release over 48 hours, with a value of 6.9% released within the first 24 hours and 7.0 and 6.9% % released at the end of the study for the (CH-co-FLP)/GLU and (CH-co-FLP)/SMP hydrogels, respectively. CONCLUSION: The novel pectin-chitosan hydrogels hold the potential to enhance the quality of life for numerous patients by minimizing the need for frequent intake of chronic medications.

Studies on Agrochemical Controlled Release Behavior of Copolymer Hydrogel with PVA Blends of Natural Polymers and Their Water-Retention Capabilities in Agricultural Soil.

Agricultural technical development relies exclusively on the effective delivery of agrochemicals and water to plants and on reducing the harmful effects of agrochemicals on useful organisms in the soil. In this study, super-absorbent hydrogels were prepared in the form of microspheres using gum Arabic (GA), which was copolymerized once with chitosan (CS) and once with poly (vinyl alcohol) (PVA). To impart mechanical strength to the hydrogel microspheres, a covalent cross-linker (N,N'-methylenebisacrylamide (MBA)) was used for the PVA/GA hydrogel, and an ionic cross-linker (sodium hexametaphosphate (SHMP)) was used for the CS/GA hydrogel. The prepared PVA/GA-CH and CS/GA-PH hydrogel microspheres showed different degrees of swelling (DSs) in the following solution media: deionized water (DW), river water (RW), and buffered solutions (pH 4; pH 9). The PVA/GA-CH hydrogel microspheres showed a maximum DS of 84 g/g in the RW, while the CS/GA-PH hydrogel microspheres showed a maximum DS of 63 g/g in the buffered solution at a pH 9. The water-retention capabilities of the hydrogels were studied using a mixture of 0.5% (w/w) hydrogel microspheres in agricultural soil; the composite showed an additional 20 days of water retention in comparison with a control sample consisting of soil alone. The hydrogels were loaded with urea, which is an important fertilizer in the field of agriculture. The PVA/GA-CH hydrogel microspheres showed a maximum loading percentage (Lmax%) of 89% (w/w), while the CS/GA-PH hydrogel microspheres showed an Lmax% = 79.75% (w/w) for urea. The urea-release behaviors of the hydrogel microspheres were studied under different release media and temperature conditions. In practice, the PVA/GA-CH hydrogel microspheres showed a better release profile in the RW at 10 °C, while the CS/GA-PH hydrogel microspheres showed a more controlled release in media at a pH 9 and at 30 °C. The urea-loaded microspheres, aside from those following the release, were characterized via FTIR and SEM. In contrast, virgin microspheres were characterized using XRD,1H NMR, (TGA and DSC), and the maximum degree of swelling, in addition to being subjected to SEM and FTIR analyses.

Effects of Surface Morphology and Type of Cross-Linking of Chitosan-Pectin Microspheres on Their Degree of Swelling and Favipiravir Release Behavior.

The cross-linked microspheres were prepared and loaded with Favipiravir SARS-CoV-2 antiviral drug, by copolymerization of chitosan (CS) with a polysaccharide extracted from fresh pomegranate peels. Moreover, glutaraldehyde (Glu) has been used as a chemical cross-linker and sodium hexametaphosphate (SHMP) as a physical cross-linker. The extracted polysaccharide was analyzed, and different techniques have been used. The analyses lead to the conclusion that it is pectin. The surface morphology of the prepared microspheres was studied using a scanning electron microscope, where the size and shape factor (S) of the Glu microspheres showed high values (74.27 µm) and (0.852), respectively, meaning their surfaces tend to be rough, whereas the SHMP microspheres showed a smaller size particle (20.47 µm) and a smaller shape factor (0.748), which gives an indication that the SHMP microspheres have smooth surfaces. The swelling studies have shown that Glu microspheres have a higher degree of swelling, which means SHMP microspheres are more compact. The prepared microspheres have shown a higher loading percentage of Favipiravir antiviral drug in SHMP microspheres (37% w/w) in comparison with Glu microspheres (35% w/w), where the electrostatic interaction between the Favipiravir ions and SHMP anions helps for more loading. The microspheres prepared under different types of cross-linking have shown initial burst release of Favipiravir, followed by a step of controlled release for a certain period of time, whose period depends on the pH of the release medium. Both Glu and SHMP cross-linked microspheres have shown high controlled release times in buffered release solutions at pH = 7.4 and for shorter periods at pH = 1.3 and pH = 9.4, which may be related to the type of electrostatic interactions between drug and polymer systems and their reactions with release solution ions.

Glutaraldehyde cross-linked chitosan microspheres for controlled release of centchroman.

Glutaraldehyde cross-linked chitosan microspheres were prepared for controlled release of centchroman, a nonsteroidal contraceptive. The cross-linked microspheres with low-molecular-weight (LMW) chitosan (260 kg mol(-1)) have shown maximum degree of swelling (287 wt%) but were found to be poor in loading and release behavior for centchroman. The microspheres with medium-molecular-weight (MMW) chitosan (1134 kg mol(-1)) have shown 250 wt% degree of swelling and 37.5 wt% loading of centchroman, but microspheres with high-molecular-weight (HMW) chitosan (2224 kg mol(-1)) have shown a low degree of swelling (150 wt%) and centchroman loading (30 wt%). The microspheres with MMW chitosan have released 82 wt% of loaded centchroman in a controlled release manner within a period of 70 h in comparison to low- (260 kg mol(-1)) and high-MW (2224 kg mol(-1)) chitosan microspheres. The chitosan microspheres with 62 wt% degree of deacetylation (DDA) were more efficient in the controlled release of centchroman in comparison to chitosan microspheres with low (48 wt%) and high-DDA (75 wt%). The fractional release of centchroman (M(t)/M(infinity)) from chitosan microspheres was used to predict the mechanism of drug release and to determine the diffusion constant (D) of centchroman.

Preparation and characterization of sodium hexameta phosphate cross-linked chitosan microspheres for controlled and sustained delivery of centchroman.

The cross-linked microspheres using chitosan with different molecular weights and degree of deacetylation have been prepared in presence of sodium hexameta polyphosphate (SHMP) as physical cross-linker. The degree of cross-linking through electrostatic interactions in chitosan microspheres has been evaluated by varying the charge density on chitosan and varying degree of dissociation of sodium hexameta polyphosphate by solution pH. The degree of deacetylation and molecular weight of chitosan has controlled electrostatic interactions between hexameta polyphosphate anions and chitosan, which played significant role in swelling, loading and release characteristics of chitosan microspheres for centchroman. The microspheres prepared by hexameta polyphosphate anions cross-linker were compact and more hydrophobic than covalently cross-linked microspheres, which has been attributed to the participation of all amino groups of chitosan in physical cross-linking with added hexameta polyphosphate anions. The microspheres prepared under different experimental conditions have shown an initial step of burst release, which was followed by a step of controlled release for centchroman. The extent of drug release in these steps has shown dependence on properties of chitosan and degree of cross-linking between chitosan and added polyanions. The degree of swelling and release characteristics of microspheres was also studied in presence of organic and inorganic salts, which shown significant effect on controlled characteristics of microspheres due to variations in ionic strength of the medium. The initial step of drug release has followed first order kinetics and become zero order after attaining an equilibrium degree of swelling in these microspheres. The microspheres prepared using chitosan with 62% (w/w) degree of deacetylation and molecular weight of 1134kgmol(-1) have shown a sustained release for centchroman for 50h at 4% (w/w) degree of cross-linking with SHMP.

Glutaraldehyde and glyoxal cross-linked chitosan microspheres for controlled delivery of centchroman.

Glutaraldehyde and glyoxal cross-linked microspheres were prepared using chitosan with different molecular weights (MWs) and degrees of deacetylation (DDAs) for sustained release of centchroman under physiological conditions. The DDA in chitosan was determined by different methods, and the samples were categorized as chitosan with low (48%), medium (62%), and high (75%) DDA. The size and shape of the microspheres were determined by scanning electron microscopy (SEM), and hydrophobicity was determined by adsorption of Rose Bengal dye on microspheres cross-linked with glutaraldehyde or glyoxal. The effect of MW, DDA, and degree of cross-linking in microspheres was studied on the degree of swelling, as well as by the loading and release of centchroman. The glyoxal cross-linked microspheres were more compact and hydrophobic and showed better sustained release in companion to chitosan microspheres and glutaraldehyde cross-linked microspheres. The linear fractional release of centchroman with the square root of time indicated a Fickian behavior of centchroman, and the microspheres also showed zero-order release kinetics for centchroman.