Current Applied Materials - Current Issue

This study aimed to identify the potential release of the drug from the tablet dosage form using Carbopol-934 and Guar Gum polymers at different concentration ratios.

The objective of this study was to determine the cumulative percentage of ciprofloxacin hydrochloride released from different polymers.

We formulated ciprofloxacin hydrochloride sustained-release tablets with Carbopol-934 and Guar gum using the wet granulation method. For the formulation of sustained-release ciprofloxacin hydrochloride tablets, both polymers were mixed in varying ratios. The tablets were examined for pre-formulation studies, including the angle of repose, bulk density, compressibility index, and physiological properties, such as variations in weight, friability, and drug content. For post-formulation studies, such as the in vitro study, the in vitro release of the drugs was evaluated in a phosphate buffer solution (pH 7.4) for 8 h. However, the physiological properties of ciprofloxacin hydrochloride tablets were limited due to their liberality.

The tablets containing guar gum (Batches B-I and B-II) showed better drug content than other polymer-based batches, such as Carbopol-934 (Batch A-I, A-II) and a mixture of both polymer Carbopol-934 and Guar gum (Batch C-I, C-II). Sustained drug release was observed in the guar gum polymer-based tablets (Batch B-II). It was observed that the dissolution profile of ciprofloxacin hydrochloride tablets formed using different polymers showed an increase in the polymer ratio, which can be related to the increase in drug release.

From this study, we can conclude that the ciprofloxacin hydrochloride drug release percentage was maximum when guar gum polymer was used in the tablet dosage form.

Cardiac arrhythmia is a health concern, requiring effective medication for proper treatment. Diltiazem hydrochloride (DTZ.HCL), a class IV anti-arrhythmic calcium channel blocker, was used as a model drug due to its ability to block Ca⁺⁺ channels in the SA and AV nodes, reducing calcium entry into cardiac cells and subsequently decreasing the force of contraction and oxygen consumption by the heart. Despite its good oral absorption, DTZ.HCL bioavailability is reduced to approximately 40% due to extensive first-pass metabolism. A nano-enabled drug delivery system has the advantage of incorporating both lipophilic and hydrophilic drugs with improved physical stability and enhanced bioavailability.

The objective of this study was to develop a solid-lipid formulation utilizing diltiazem hydrochloride and evaluate it for its bioavailability enhancement.

In the experimental study, SLNs were prepared using the microemulsion technique. A blend ratio (1:1) of lipid (stearic acid: compritol 888 ATO), span 80, PEG 200, and water was selected based on the microemulsion region obtained from the Triplot (4.1) ternary phase diagram. The hydrophilic drug diltiazem hydrochloride was incorporated into the lipid blend, and a preheated Smix was maintained at 80°C to obtain a transparent microemulsion, which then crystallized to form SLNs upon subsequent dispersion in cold water (1:25). Critical process parameters, including magnetic stirring speed, homogenizer speed, and probe sonication cycle, were optimized using Design Expert 10 software to achieve the desired particle size diameter, PDI, and entrapment efficiency.

The results revealed that the particle size and PDI were significantly influenced by the span 80 and PEG 200. An increase in the concentration of the lipid blend resulted in large particle sizes. The optimized formulation showed a particle size of 415.4 ± 0.2 nm, PDI of 0.184 ± 0.01, and zeta potential of -24.19 ± 0.12 mV. These results were corroborated by DSC thermograms, which indicated reduced enthalpy associated with the reduced particle size of SLNs. Given that diltiazem hydrochloride is a hydrophilic drug with high water solubility, the entrapment efficiency was relatively 30.6% ± 0.45. In vitro release studies demonstrated an initial burst release, followed by a sustained release of 85% over 24 hours. The optimized SLNs followed the Higuchi matrix model, with a coefficient of correlation (R²) value of 0.9369.

Results concluded successful development of SLNs with improved bioavailability when compared by way of in-vitro method with marketed preparations.

To bring new materials with high performance, a large number of composites, among others, such as starch-laminated double hydroxides (Starch/ZnCr-LDH), have been produced, which have shown significant adsorption predisposition to remove heavy metals and dyes. These LDHs display great adsorption potential due to their high anion exchange capacity, large surface area, and good thermal stability.

This study aimed to develop starch-ZnCr-hydroxide composite (S/ZnCr-LDH) as a new material and investigate its performance in removing various anionic dyes compared to ZnCr-LDH.

The starch-ZnCr-laminated double hydroxides (S/ZnCr-LDH) and ZnCr-LDH composites were prepared by the co-precipitation method and their structures were characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), differential thermogravimetric/thermal analysis (TG/DTA) Scanning electron microscopy (SEM), and Energy Dispersive X-rays Spectroscopy (EDX).

The effects of different operating parameters, such as pH, initial CR concentration, contact time, and adsorbent dose, on CR removal were studied. The results showed that the S/ZnCr-LDH composite is more efficient for CR removal, reaching 99% at pH 3, while ZnCr-LDH presented a removal efficiency of 90%. Isothermal data were processed according to the Langmuir, Freundlich, and Temkin models. According to the results, Langmuir's isothermal model best matched the experimental data, with a maximum adsorption capacity of 252.92 and 236.98 mg/g for S/ZnCr-LDH and ZnCr-LDH, respectively. The adsorption kinetics corresponded to the PSO model. CR dye molecules were adsorbed to different sites on the S/ZnCr-LDH composite based on various interactions, such as electrostatic interactions, hydrogen bonds, and Van der Waals forces.

S/ZnCr-LDH composite displays the highest capacity to remove CR dye molecules compared to ZnCr-LDH.

To deliver the drug through the pulmonary route, polymers like oleoyl-carboxymethyl chitosan (O-CMC), chitosan, and HPMC (hydroxypropyl methylcellulose) K4M are well known for their effective mucoadhesive properties. Drug-loaded polymeric nanoparticles have the potential for a therapeutic response for the targeted site is a beneficial approach.

The present study is to develop polymeric nanoparticles (PNPs) utilizing mucoadhesive polymers with varying concentrations as well as to develop the PNPs for pulmonary delivery.

Polymeric nanoparticles are developed by homogenization and solvent evaporation methods and characterized by modified twin-stage impinger to study in vitro deposition.

The characterization of pirfenidone-loaded polymeric nanoparticles (PFD-PNPs) reveals that the mean particle size of O-CMC-PNPs is 140.8 nm ± 20, found to be less than CS-PNPs and HPMC-PNPs. The polydispersibility index reveals that the particles of all prepared formulations are homogenous. At the same time, the zeta potential of O-CMC-PNPs is 40.8 mV ± 5.64, and the entrapment efficiency is 91% ± 1.2, which is better as compared to Chitosan and HPMC K4M PNPs and makes them efficient for pulmonary delivery. Findings from the in vitro deposition study using modified TSI show that 88.5% of the drug delivered through nebulization from both the stage of right and left sides of the TSI suggests effective deposition in the lungs of O-CMC PNPs, and it may move to the deeper regions because of the lowest diameter of the particles. Sustaining release of the drug was found in the O-CMC PNPs for 8 hours, compared with 5 and 7 hours for HPMC PNPs and Chitosan PNPs, respectively.

Overall, the results of the O-CMC-PNPs highlight that the prepared nanoparticles with O-CMC would be effective for pulmonary delivery instead of chitosan and HPMC K4M.