Nazar Mohammad Ranjha

Preparation and characterization of hybrid pH-sensitive hydrogels of chitosan-co-acrylic acid for controlled release of verapamil

In the present work crosslinked hydrogels based on chitosan (CS) and acrylic acid (AA) were prepared by free radical polymerization with various feed compositions using N,N methylenebisacrylamide (MBA) as crosslinking agent. Benzoyl peroxide was used as catalyst. Fourier transform infrared spectra (FTIR) confirmed the formation of the crosslinked hydrogels. This hydrogel is formed due to electrostatic interaction between cationic groups in CS and anionic groups in AA. Prepared hydrogels were used for dynamic and equilibrium swelling studies. For swelling behavior, effect of pH, polymeric and monomeric compositions and degree of crosslinking were investigated. Swelling studies were performed in USP phosphate buffer solutions of varying pH 1.2, 5.5, 6.5 and 7.5. Results showed that swelling increased by increasing AA contents in structure of hydrogels in solutions of higher pH values. This is due to the presence of more carboxylic groups available for ionization. On the other hand by increasing the chitosan content swelling increased in a solution of acidic pH, but this swelling was not significant and it is due to ionization of amine groups present in the structure of hydrogel. Swelling decreased with increase in crosslinking ratio owing to tighter hydrogel structure. Porosity and sol-gel fraction were also measured. With increase in CS and AA contents porosity and gel fraction increased, whereas by increasing MBA content porosity decreased and gel fraction increased. Furthermore, diffusion coefficient (D) and the network parameters i.e., the average molecular weight between crosslinks (Mc), polymer volume fraction in swollen state (V2s), number of repeating units between crosslinks (Mr) and crosslinking density (q) were calculated using Flory-Rehner theory. Selected samples were loaded with a model drug verapamil. Release of verapamil depends on the ratios of CS/AA, degree of crosslinking and pH of the medium. The release mechanisms were studied by fitting experimental data to model equations and calculating the corresponding parameters. The result showed that the kinetics of drug release from the hydrogels in both pH 1.2 and 7.5 buffer solutions was mainly non-Fickian diffusion.

Synthesis and Characterization of Chemically Cross-Linked Acrylic Acid/Gelatin Hydrogels: Effect of pH and Composition on Swelling and Drug Release

This present work was aimed at synthesizing pH-sensitive cross-linked AA/Gelatin hydrogels by free radical polymerization. Ammonium persulfate and ethylene glycol dimethacrylate (EGDMA) were used as initiator and as cross-linking agent, respectively. Different feed ratios of acrylic acid, gelatin, and EGDMA were used to investigate the effect of monomer, polymer, and degree of cross-linking on swelling and release pattern of the model drug. The swelling behavior of the hydrogel samples was studied in 0.05 M USP phosphate buffer solutions of various pH values pH 1.2, pH 5.5, pH 6.5, and pH 7.5. The prepared samples were evaluated for porosity and sol-gel fraction analysis. Pheniramine maleate used for allergy treatment was loaded as model drug in selected samples. The release study of the drug was investigated in 0.05 M USP phosphate buffer of varying pH values (1.2, 5.5, and 7.5) for 12 hrs. The release data was fitted to various kinetic models to study the release mechanism. Hydrogels were characterized by Fourier transformed infrared (FTIR) spectroscopy which confirmed formation of structure. Surface morphology of unloaded and loaded samples was studied by surface electron microscopy (SEM), which confirmed the distribution of model drug in the gel network.

Drug release optimization from microparticles of poly(E-caprolactone) and hydroxypropyl methylcellulose polymeric blends: formulation and characterization

In this study, polymeric blend microparticles are prepared with tunable drug releasing behavior, imparted by using poly(e-caprolactone) (PCL) as hydrophobic and hydroxypropyl methylcellulose (HPMC) as hydrophilic biodegradable polymeric constituents. Microparticles were prepared by simple oil in water emulsion-solvent evaporation method and evaluated for their sustained release profile by using nifedipine (half-life is about 2 h) as model drug. Hydrophilic PCL is added to optimize the drug release in simulated aqueous body fluid. Polyvinyl alcohol (PVA), used as emulsifier, was found to improve shape while HPMC increased surface smoothness of microparticles. High encapsulation efficiency was achieved, controllable by HPMC concentration. In vitro dissolution studies in acidic and neutral pH showed sustained release profile for all formulations. Synthesized microparticles, provided control over hydrophobic drug release by changing the proportion of HPMC and PCL in formulation at both acidic and intestinal pH.

Swelling and Aspirin Release Study: Cross-Linked pH-Sensitive Vinyl Acetate-co-Acrylic Acid (VAC-co-AA) Hydrogels

The objective of this work was to develop new pH-sensitive hydrogels to deliver gastric mucosal irritating drugs to the lower part of the gastrointestinal tract. For this purpose, cross-linked vinyl acetate-co-acrylic acid (VAC-co-AA) hydrogels were synthesized by using N, N, methylene bisacrylamide (MBAAm) as a cross-linking agent. Different ratios of 90:10, 70:30, 50:50, 30:70, and 10:90 of VAC-co-AA were synthesized. All of the compositions were cross-linked using 0.15, 0.30, 0.45, and 0.60 mol percent MBAAm. Swelling and aspirin release were studied for 8 hour period. The drug release data were fitted into various kinetic models like the zero-order, first-order, Higuchi, and Peppas. Hydrogels were characterized by Fourier transform infrared spectroscopy and scanning electron microscopy. In addition to the above, these hydrogels were loaded with 2%, 8% and 14% w/v aspirin solutions, keeping the monomeric composition and degree of cross-linking constant. In conclusion, it can be said that aspirin can be successfully incorporated into cross-linked VAC/AA hydrogels and its swelling and drug release can be modulated by changing the mole fraction of the acid component in the gels.

Enhanced gastric retention and drug release via development of novel floating microspheres based on Eudragit E100 and polycaprolactone: synthesis and in vitro evaluation

Abstract Eudragit E 100 and polycaprolactone (PCL) floating microspheres for enhanced gastric retention and drug release were successfully prepared by oil in water solvent evaporation method. Metronidazole benzoate, an anti-protozoal drug, was used as a model drug. Polyvinyl alcohol was used as an emulsifier. The prepared microspheres were observed for % recovery, % degree of hydration, % water uptake, % drug loading, % buoyancy and % drug release. The physico-chemical properties of the microspheres were studied by calculating encapsulation efficiency of microspheres and drug release kinetics. Drug release characteristics of microspheres were studied in simulated gastric fluid and simulated intestinal fluid i.e., at pH 1.2 and 7.4 respectively. Fourier transform infrared spectroscopy was used to reveal the chemical interaction between drug and polymers. Scanning electron microscopy was conducted to study the morphology of the synthesized microspheres.

The Structural, Crystallinity and Thermal Properties of pH responsive Interpenetrating Gelatin/Sodium Alginate Based Polymeric Composites for the Controlled Delivery of Cetirizine HCl

Objectives: The present work aimed to design and synthesize pH-sensitive cross-linked Ge/SA hydrogels using different ratios of each polymer, and to investigate the effect of each polymer on dynamic, equilibrium swelling, and in vitro release pattern of cetirizine hydrochloride, which was selected as a model drug. Materials and Methods: These gelatin and sodium alginate hydrogels were prepared at room temperature through free radical polymerization using glutaraldehyde as a crosslinker. These polymeric composites were used as model systems to envisage various important characterizations. The in vitro release pattern of drug was investigated in three different mediums (phosphate buffer solution of pH 1.2, 5.5, 7.5 whose ionic strength was kept constant). Various structure property relationships that affect its release behavior were determined such as swelling analysis, porosity, sol-gel analysis, average molecular weight between crosslinks (Mc), solvent interaction parameter (χ), volume fraction of polymer (V2,s) and diffusion coefficient. The structural, crystallinity, and thermal stability were confirmed using FTIR, XRD, and DSC analysis. Results: These hydrogels showed maximum swelling at pH 1.2. Zero-order, first-order, Higuchi, and Peppas models were applied to demonstrate the release pattern of drug. The release of drug occurred through non-Fickian diffusion or anomalous mechanism. Porosity was found increased with an increase in concentration of both polymers, and porosity decreased when the concentration of the crosslinker was increased. Gel fraction increased with an increase in concentration of SA, Ge, and glutaraldehyde. Conclusion: The prepared pH sensitive hydrogels can be used as a potential carrier for the sustained delivery of cetirizine hydrochloride.