Investigations of process parameters during dissolution studies of drug loaded 3D printed tablets

The present research paper attempts to study the effect of different process parameters on the dissolution rate during 3D printed tablets. Three-dimensional printing has the potential of serving tailored made tablets to cater personalized drug delivery systems. Fluorescein loaded PVA filaments through impregnation route was used to fabricate tablets based on Taguchi based design of experimentation using Fused Deposition Modelling (FDM). The effect of print speed, infill percentage and layer thickness were analyzed to study the effect on rate of dissolution. Infill percentage followed by print speed were found to be critical parameters affecting dissolution rate. The data analysis provided an insight into the study of interaction among different 3D printing parameters to develop an empirical relation for percentage release of the drug in human body.

FORMULATION DEVELOPMENT AND EVALUATION OF FAST DISSOLVING FILMS OF EBASTINE

Objective: To overcome the limitations of fast dissolving tablets, a novel fast dissolving film of ebastine was formulated for attaining quick onset of action, aiding in the enhancement of bioavailability favorable in severe conditions of allergies. Methods: Films of ebastine were prepared by the solvent casting method using hydroxypropyl methylcellulose E-15, hydroxypropyl methylcellulose K-4 as a film base with different concentrations of crospovidone as superdisintegrant and polyethylene glycol-400 as a plasticizer. Further physical characteristics such as uniformity of weight, thickness, and drug content uniformity, tensile strength, folding endurance, percentage elongation, surface pH, disintegration and in vitro drug release were evaluated. Results: The optimized formulations with film base hydroxypropyl methylcellulose E-15 and hydroxypropyl methylcellulose K-4 containing 8% crospovidone showed 99.34 % and 97.42 % of maximum cumulative percentage release respectively exhibiting first order kinetics. However, no significant change was observed in stability studies. Conclusion: The concept of formulating fast dissolving films of ebastine offers a suitable approach in exhibiting rapid onset of action with improved delivery.

CEFPODOXIME PROXETIL FAST DISSOLVING TABLETS: COMPARATIVE STUDY

Objective: In the present investigation, fast dissolving tablets of cefpodoxime proxetil were formulated using superdisintegrants to impart fast disintegration. Methods: In the current study, 12 formulations of fast dissolving tablets of cefpodoxime proxetil were formulated using two different approaches viz., direct compression and sublimation. Three different superdisintegrants viz., croscarmellose sodium, sodium starch glycolate, and crospovidone were used in a different concentration in all the respective formulations. The final powder blend was subjected for the pre-compression evaluation and all the formulations were evaluated for post-compression parameters. Stability studies were also evaluated for the best formulations as per ICH guidelines. Finally, results were statistically analyzed by the application of one way ANOVA test and t-test. Results: Among all the formulations of different approaches, formulation cefpodoxime proxetil 4 (CP4) containing 6% crospovidone as a super disintegrant was showed the best results. In vitro dissolution data revealed that formulation CP4 prepared by direct compression method showed 99.387±0.270% drug release within 15 min whereas the percentage release by formulation prepared by using sublimation showed 83.927±0.735% release. The optimized formulation was further subjected to comparative in vitro study with two marketed formulation of different brands. Conclusion: All the data of all formulations is shows that direct compression approach is the best approach for developing the fast dissolving tablets to enhance the onset of action and bioavailability.

Dendrimer-Functionalized Hybrid Materials Based on Silica as Novel Carriers of Bioactive Acids

One of the major goals in the materials science is the design and development of non-toxic, versatile, and efficient drug delivery systems. The study reported in this paper concerns the syntheses of poly(amidoamine) (PAMAM) dendrimers with tris(2-aminoethyl)amine as an amine core and different terminal amines, and their attachment to silica matrix. The obtained ethylenediamine (EDA), triethylenetetramine (TETA), tris(2-aminoethyl)amine (TREN) and 4,7,10-trioxa-1,13-tridecanediamine (TRI-OXA) dendrimers were introduced to the support surface via an epoxy linker, leading to a loading efficiency in the range of 0.054–0.113 mmol g−1, determined using elemental and thermogravimetric analyses. The materials exhibited high adsorption capacities towards the chosen model drugs: folic, salicylic and nicotinic acid. The investigated adsorption processes were found to follow the Freundlich isotherm model, with indication of the drugs’ structure influence on the binding efficiency. Drug-loaded hybrid materials were also described for in vitro drug release in three pH-different paraphysiological media. The highest percentage release was obtained in the tests performed at pH 2.0, ranging between 35.42 and 99.83%. Satisfactory results and the versatility of PAMAM dendrimers may lead to the application of such materials not only as drug carriers dedicated to a wide range of pharmaceutics, but also as analytical tools for pre-concentration and/or the determination of biocompound contamination in samples.

Effect of Different Pressure-Sensitive Adhesives on Performance Parameters of Matrix-Type Transdermal Delivery Systems

Matrix-type transdermal delivery systems (TDS) are comprised of the drug dissolved or dispersed in a pressure-sensitive adhesive (PSA) matrix and are designed to provide a controlled delivery through the skin and into systemic circulation. PSAs can directly affect the permeation, release, and performance characteristics of the system. In this study we aimed to design and characterize transdermal delivery systems formulated with lidocaine—as the model drug—loaded in different PSAs, including silicone, polyisobutylene (PIB), and acrylate. TDS containing lidocaine at its saturation points were prepared by the solvent casting method. In vitro permeation studies across dermatomed porcine ear skin were performed using Franz diffusion cells. In vitro release studies were carried out using USP apparatus 5 (paddle over disk). The cumulative amount permeated from the acrylate was significantly higher than silicone and PIB. The acrylate TDS contained a ten times higher drug amount than silicone TDS, but the permeation flux was only two folds higher. Results also showed the release of drug does not linearly correlate to saturation, as the silicone TDS comprising of the lowest amount of drug loading, showed the highest percentage release indicating the choice of PSA affected the drug release and permeation profile.

DEVELOPMENT AND IN VITRO EVALUATION OF 5-FLUOROURACIL NANOPARTICLES BY SALTING OUT TECHNIQUE

Objectives: At the current miserable state of the prevalence of cancers, there is a need for the development of simple technologies to prepare formulations of anticancer drugs with less economy and investment. Hence, the aim of the present work is to prepare nanoparticles of 5-fluorouracil (5-FU) by simple technique, such as salting out method. Methods: Nanoparticles containing 10 mg of 5-FU were prepared by salting out method using Eudragit-100 as polymer. The prepared nanoparticles were evaluated by particle size, zeta potential, in vitro drug release studies, and drug-excipient interaction studies. Results: Nanoparticles prepared by salting out methods showed higher dissolution rate for formulation F3 and F5 revealed high percentage release of 98.6±0.24 in 60 min and 86.5±0.39% in 120 min. Fourier transform infrared (FTIR) spectra revealed no interaction between drug and excipients used for preparation. Conclusion: 5-FU nanoparticles can be produced successfully by salting out method using drug to polymer (Eudragit S-100) ratio of 1:3 to possess ideal drug release characteristics and average particle size of 205.1 nm.

Application of Eudragit RS 30D as a Potential Drug Release Retardant of Acetaminophen and Caffeine for Prolonged Duration of Comfort

The objective of the study is to formulate an extended release matrix tablet dosage form containing acetaminophen and caffeine by applying polymer technology which will relieve all kinds of pain for about 12 hours. Considering the fact that there is no such formulation available in the pharmaceutical market, it is expected that this drug could be an effective introduction. Hydrophobic polymers have a great application in pharmaceutical sciences as they retard the release of water-soluble drugs and give prolonged effect. Eudragit RS 30D was used to prepare 3 formulations (EF1, EF2, and EF3) containing varying concentrations of polymer, through the wet granulation method. Each tablet contained 1000 mg of acetaminophen and 130 mg of caffeine including other suitable excipients. All pharmacopeial and nonpharmacopeial tests were conducted to determine the quality of dosage form and to identify optimized formulation among EF1-EF3. Dissolution was conducted on similar gastric conditions through which different kinetic models were applied using DDSolver. For 12 hrs of dissolution, caffeine was released from EF1, EF2, and EF3 with the percentage release in the range from 99.85% to 100.65%, 99.32% to 100.28%, and 98.09% to 100.77%, respectively. For acetaminophen, the percent release was from 99.81% to 100.91%, 100.24% to 100.91%, and 86.81% to 95.73% for EF1-EF3, respectively. Results concluded that EF2 is the most optimized drug having all physicochemical quality control tests within the specified limits. On applying different models like zero-order, Hixson-Crowell, Higuchi, and Korsmeyer-Peppas upon use, it is concluded that the formulation follows Korsmeyer-Peppas as it was the best-fitted model with the r2 value closest to 0.999. EF2 is considered as a potential drug to be manufactured that will give prolonged relief against pain and will decrease compliance issues related to dosing frequency.

Formulation and Evaluation of Fluvoxamine Maleate Loaded Lipid Nanoparticle

Recently solid lipid nanoparticles (SLN's) have been received much attention by the researchers owing to its biodegradability, bioavailability and the ability to deliver wide range of drugs to the targeted site of action. The purpose of the present study is to develop and evaluate the fluvoxamine maleate loaded lipid nanoparticles. The fluvoxamine maleate lipid nanoparticles (LN’s) were prepared by the hot melt homogenization followed by the sonication by using different combination of lipids like tristearin, compritol, olive oil, coconut oil, sesame oil. Compatibility study was confirmed by FTIR and DSC. The LN’s were evaluated for particle size, PDI, zeta potential, entrapment efficiency and in-vitro drug release. For the Fluvoxamine maleate LN’s prepared using the solid lipids, the particle size ranged from 98.58 to 152.43 nm. PDI of all formulations were good within the range of 0.239 to 0.456 with zeta potential from - 6.52 to -18.6 mV. Entrapment efficiency observed was in the range of 64.56 to 84.23 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 46.14 to 81.48%. For the formulations prepared using the combination of solid lipids and liquid lipids, Fluvoxamine maleate LN’s the particle size ranged from 63.22 to 263.8 nm. With good PDI range from 0.229 to 0.514 Zeta potential of all formulation is from - 5.01 to -9.30 mV. Entrapment efficiency observed was in the range of 71.02 to 90.51 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 63.71 to 85.41% depending upon the drug lipid ratio, the type of lipid used. The release kinetic studies showed that the release was first order, diffusion controlled, and the ‘n’ values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Anomalous (non-Fickian) diffusion type.

ANTIOXIDANT AND ANTIMICROBIAL ACTIVITIES OF CITRUS LEMON PEELS ENCAPSULATED IN PVA

In this study, waste lemon peels were converted into a dietary supplement. Lemon peels were used because of the abundance of phytochemicals present in it and also they are easily available throughout the year. To improve the therapeutic efficacy, we used Polyvinyl Alcohol (PVA) as a nanocarrier of lemon peel methanolic extract. The lemon peel extract was encapsulated in PVA by the solvent evaporation method, to improve the solubility and stability of the compounds in the extract. Characterization of the prepared lime peel nanoformulation (LP-NF) was done by Scanning Electron Microscope, Zeta potential and Fourier Transform Infrared techniques. The antioxidant assays like DPPH(2,2-diphenyl-1- picrylhydrazyl) radical scavenging assay and hydrogen peroxide assay showed a high scavenging activity when compared with commercial supplement with the IC50 value of 24 ± 0.05 and 26.07 ± 0.11 respectively. The Gram-negative bacteria, E. coli showed a zone of inhibition of 18 mm indicating the antibacterial property of LP-NF. The percentage release of the nanoformulation from sodium alginate beads was calculated and it showed the release of nanoparticle up to 83% after 7 hours in PBS at pH 7.4

FORMULATION AND EVALUATION OF METRONIDAZOLE TABLETS USING NATURAL GUM

Objectives: The objective of the present study was to formulate the metronidazole tablets using natural Aloe vera gum as binding agent. Materials and Methods: To determine the binding properties of the extracted A. vera gum were used for the preparation of metronidazole tablets and compared with other binding agents such as acacia and sodium carboxymethyl cellulose (CMC). Physical properties such as hardness, friability, disintegration time, and in vitro dissolution rate are the important parameter which determines for each formulation. Three batches of metronidazole tablets are prepared using acacia (F1), sodium CMC (F2), and A. vera gum (F3) as binding agent. Results: The granules were evaluated by determining the angle of repose (26.01 ± 0.110–27.18 ± 0.166°), bulk density, tapped density, Hausner ratio, and Carr’s index. It shows satisfactory results. At time 90 min, the percentage release of drug for F1, F2, and F3 was 44.947%, 31.467%, and 53.424%, respectively. The tablets prepared with A. vera gum showed faster release profile than other binders. Conclusion: From the results, it was shown that tablets prepared with A. vera gum have good binding properties and also helped tablets for faster release.