Biopolymer based film loaded with Cholecalciferol: A novel technique to enhance nutritional supplement absorbance.

In terms of delivery systems for active compounds, orally disintegrating films are a great option. The initial stage in creating an oral disintegrating film is selecting a film-forming polymer. The basic polymers combination Microcrystalline Cellulose (MCC), which is co-processed with Carboxymethylcellulose Sodium (CMC) and hydroxypropylmethyl cellulose were used to create an oral disintegrating film that contains cholecalciferol (Vitamin D3), a fat-soluble vitamin that aids in the body's absorption of calcium and phosphorus. The goal of the current inquiry was to develop orally disintegrating films of vitamin D3 to improve patient comfort and compliance for pediatric or elderly patients due to its simplicity of administration. Films containing drugs and made of the appropriate plasticizer and chosen polymers demonstrated outstanding film forming and folding endurance. The dissolution test showed that Vitamin D3 has a rapid disintegration property, with the majority of it dissolving in the medium (pH 6.8) in less than two minutes after being inserted. To verify that the films were successfully formed, a variety of procedures including HPLC, FT-IR and microscopic studies were employed. When kept at 40oC with humidity of 75%, the film showed good stability for at least three months.

An evaluation of spectral and statistical parameters of ion pair complexation of Zafirlukast using chromogenic dyes in solid dispersion-based formulations.

The purpose of present work was to develop a novel analytical method for orally given leukotriene antagonist Zafirlukast (ZST), present in Meglumine and Eudragit EEPO based solid dispersion formulation. Four simple, extraction-free, fast, and economical methods based on charge transfer complexation among nitrogen of ZST with sulfonyl group comprising chromogenic mediator bromophenol blue (BPB-Method B), bromothymol blue (BTB-Method C) and bromocresol green (BCG-Method D). The first method (A) is based on the analysis using 0.1 M HCl as a solvent at λmax 242 nm while chromogenic methods yield color complex at λmax 415 nm (BPB-Method B), λmax 420 nm (BTB-Method C) and λmax 435 nm (BCG-Method D). The Beer's Law stayed linear in the concentration ranges of 1-10, 10-75, 5-40 and 15-100 µg/ml for methods A, B, C and D, respectively. The spectral and thermodynamic characterization of each method was carried out by the application of Molar Absorptivity, LOD, LOQ, Association Constant and Gibbs free energy (ΔGo). The methods were statistically optimized and evaluated by F-Distribution Value, P-Value, Shapiro-Wilk P-Value, regression analysis, Q-Q plot, prediction interval, residual histogram and plots. Various experimental conditions affecting the complexation and stability of chromogenic complexes are cautiously studied including optimal temperature, chromogenic agent volume, color stability, recovery, precision and accuracy. All the measurements were executed under ICH guidelines. It can be established that proposed would be an appropriate prospective analytical approach for estimation of ZST in pure bulk, solid dispersions and dosage forms.

Synthesis of calcium carbonate-quince bio-composite for programmed and on-demand drug release of paracetamol at target site: a green chemistry approach.

In this study, an inorganic-organic composite system was developed through biomineralization of calcium carbonate in the quince-seed mucilage-based hydrogel. Drug-polymer interactions were studied by FTIR, DSC, XRD and SEM analysis. The water absorption capacity was calculated by swelling index. Drug release was determined at various pH. Several in vitro kinetic models were applied to observe drug release behaviour. Studies of drug-polymer interactions and particle flow characteristics of the developed composite material have shown that there is good compatibility between drug and the excipients. The XRD and SEM results confirmed calcite polymorphs in the developed composite material. Thermograms showed that the developed composite material was heat stable. A restricted drug release was observed in an acidic medium (pH 1.2). A controlled drug release was depicted from the developed system at pH 6.8. The drug release mechanism of Super Case II was suggested. The developed system was considered to be an effective drug carrier for colon targeted oral delivery of non-steroidal anti-inflammatory drugs (NSAIDs) to avoid gastric irritation and risk of ulceration. Graphical abstract: An illustration of extraction of quince hydrogel and development of calcium carbonate-quince (CaCO3-Q) composite system; QSM = Quince seed mucilage. Supplementary Information: The online version contains supplementary material available at 10.1007/s00289-022-04400-1.

Formulation of Modified-Release Bilayer Tablets of Atorvastatin and Ezetimibe: An In-Vitro and In-Vivo Analysis.

The objective of this work was to formulate co-loaded bilayer tablets containing ezetimibe (EZB) and atorvastatin (ATC). ATC loaded in the immediate-release (IR) layer is an HMG CoA reductase inhibitor, while EZB, added in the sustained-release (SR) layer, is a lipid-lowering agent. This study was conducted to evaluate the effects of polymer on the formulation and characterization of bilayer tablets, as well as the therapeutic impact of the concurrent use of both drugs having a sequential release pattern. To obtain the optimized results, four different formulations with variable compositions were developed and evaluated for different parameters. The drug release studies were carried out using a type II dissolution apparatus, using phosphate buffer solution (PBS) of 1.2 pH for IR of EZB for an initial 2 h, followed by 24 h studies for ATC in PBS 6.8 pH. The IR layer showed rapid drug release (96%) in 2 h, while 80% of the ATC was released in 24 h from the SR layer. Locally obtained, 6-week-old female albino rats were selected for in vivo studies. Both preventive and curative models were applied to check the effects of the drug combination on the lipid profile, atherosclerosis and physiology of different organs. Studies have shown that the administration of both drugs with different release patterns has a better therapeutic effect (p < 0.05), both in preventing and in curing hyperlipidemia. Conclusively, through the sequential release of ATC and EZB, a better therapeutic response could be obtained.

Development and optimization of metoclopramide containing polymeric patches: impact of permeation enhancers

Abstract The study is aimed to develop a monolithic controlled matrix transdermal patches containing Metoclopramide as a model drug by solvent casting method. Eudragit L100, Polyvinylpyrrolidone K-30, and Methylcellulose were used in different ratios and Polyethylene glycol 400 added as a plasticizer. Resulting patches were evaluated for their physicochemical characters like organoleptic characters, weight variation, folding endurance, thickness, swelling index, flatness, drug content, swelling index, percentage erosion, moisture content, water vapor transmission rate and moisture uptake. Formed patches were also evaluated through Fourier transform spectroscopy (FT-IR), X-ray diffraction (XRD), Differential Scanning calorimetry (DSC) and Scanning Electron Microscopy (SEM). Results of SEM unveiled smooth surface of drug-loaded patches. In-vitro dissolution studies were conducted by using dissolution medium phosphate buffer saline pH 7.4. Effect of natural permeation enhancers was elucidated on two optimized formulations (Z4 and Z9). Different concentrations (5%-10 %) of permeation enhancers i.e. Olive oil, Castor oil and Eucalyptus oil were evaluated on Franz diffusion cell using excised abdominal rat skin. Z4-O2 (Olive oil 10%) had enhanced sustain effect and flux value (310.72) close to the desired flux value. Z4-O2 followed Higuchi release model (R2= 0.9833) with non-fickian diffusion release mechanism (n=0.612)

O-Carboxymethylated chitosan; A promising tool with in-vivo anti-inflammatory and analgesic properties in albino rats.

In the present study chitosan derivative, O-carboxymethylated chitosan (O-CMC) was synthesized by simple and cost-effective technique and scrutinized for in-vivo anti-inflammatory and analgesic activities. Na-carboxymethyl intermediate was prepared by acidification of chitosan with monochloroacetic acid and neutralized with 0.5 M NaOH which was further converted into O-CMC by using 0.2 M HCl. Resulted O-CMC was confirmed by FTIR spectroscopy. Inflammation was induced in albino rats by carrageenan and anti-inflammatory property of synthesized O-CMC was confirmed by calculating paw volume, %age inflammation and %age inhibition of inflammation. Analgesic properties were confirmed by %age analgesia and latency time. The results revealed that the synthesized O-CMC derivative of chitosan showed stretched peaks at 2891 cm-1, 1631 cm-1, 1060 cm-1 of -OH, -NH and -CO respectively. Formulation V was optimized due to its of percentage inflammation, 45.5 ± 0.02% inhibition of inflammation and decrease in paw volume, as well as a positive control on % age analgesia and latency time as compared to chitosan by applying statistics. O-CMC may be considered a remarkable anti-inflammatory and analgesic agent which may provide adjunctive effect with other active pharmaceutical ingredients.

Synthesis of N,O-Carboxymethyated chitosan and its application in the development of acyclovir loaded nanoparticles.

Objective of the study was to perform a physico-chemical modification of low molecular weight chitosan (CTS) followed by its use in the formulation of nanoparticles carrier of Acyclovir (ACY). Modified polymer was used to develop ACY loaded nanoparticles in order to achieve optimal response and to minimize toxic effects of ACY. CTS were dissolved in varying concentrations of potassium hydroxide solution to synthesize N, O-carboxymethylated chitosan (N,O-CMC). Synthesized derivative was further processed with different concentrations of TPP (0.3%, 0.5% and 1%) and ACY to prepare nanoparticles. N,O-CMC and prepared formulations were characterized by Fourier transform infrared spectroscopy (FTIR). Furthermore, scanning electron microscopy (SEM) was done to observe the surface morphology, zeta size and zeta potential for particle size analysis, in vitro dissolution to find out the release pattern and kinetic modeling was done to observe the release mechanism and pattern of the drug. Result of FTIR was evidence of polymer modification when compared with chitosan which was the parent standard polymer as well as compatibility of the ingredients. Results of zeta size analysis have confirmed that the particles are of nanosized (109-125nm). Good controlled 98.77% over release of 24 h of formulation B observed in phosphate buffer of intestinal pH. Higuchi model with Fickian diffusion was dominating due to the formation of N, O-CMC complex which created smooth surface. All the results were significant and within the p value of 0.001. Conclusively, the modification of the CTS was in nanoparticle showed good sustained release.

A mechanistic evaluation of the traditional uses of Nepeta ruderalis in gastrointestinal and airway disorders.

CONTEXT: Nepeta ruderalis Buch.-Ham. (Lamiaceae), locally known as Badranj Boya, is an aromatic herb used traditionally as an antispasmodic, antidiarrhoeal, and anti-asthamatic remedy. OBJECTIVE: Aqueous methanolic extract of N. ruderalis was studied to investigate its traditional uses. MATERIALS AND METHODS: Study was conducted from September 2015 to February 2016. In vitro spasmolytic and broncho-relaxant activity of crude extract of N. ruderalis (whole plant) was evaluated at 0.01-10 mg/mL final bath concentration in isolated rabbit jejunum and tracheal tissues, using PowerLab data acquisition system (Transonic Systems Inc., Ithaca, NY). In vivo antidiarrhoeal activity was evaluated in castor oil-induced diarrhoeal mice at the dose of 300 and 500 mg of crude extract orally. RESULTS: Crude extract of N. ruderalis completely relaxed spontaneously contracting, high K+ (80 mM) and carbachol (1 µM) induced contracted jejunum with an EC50 value of 5.85 (5.45-6.27), 4.0 (3.80-4.23) and 2.86 (2.48-3.29), similar to verapamil. Nr.Cr relaxed high K+ and carbachol induced contractions, at 5 and 10 mg/mL with an EC50 value of 2.37 (2.11-2.67) and 3.26 (2.9-3.67), respectively, and also displaced calcium concentration-response curves toward right at 0.1 and 0.3 mg/mL. Nr.Cr exhibited antidiarrhoeal protection at a dose of 300 and 500 mg/kg, similar to verapamil, whereas no acute toxicity signs were seen up to 5 g/kg in healthy mice. DISCUSSION AND CONCLUSION: Results suggest the presence of spasmolytic and broncho-relaxant effects in the crude extract of N. ruderalis, possibly mediated through calcium channel-blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal and airway disorders.

DEVELOPMENT OF COMPRESSED COATED POLYPILL WITH MUCOADHESIVE CORE COMPRISING OF ATORVASTATIN/CLOPIDOGREL/ASPIRIN USING COMPRESSION COATING TECHNIQUE.

The study was conducted to formulate and assess a novel polypill comprising of atorvastatin calci- um (ATVC), clopidogrel bisulfate (CLB) and aspirin (ASP) which, after in vivo correlation, can be intended for use in hyperlipidemic chronic heart disease patients. Polypill was made by the compression coating technique (CCT) with multiple active ingredients along with different concentrations of mucoadhesive and sustained release polymers, i.e., Carbopol 934 (CAB), Methocel k15 (MTH) and sodium carboxymethyl cellulose (NaCMC). The effect of different concentration of polymers on physical properties, wash off time, mucoadhe- sion strength, swelling behavior, surface pH and drug release kinetics were investigated. In vitro drug release studies showed that combination of CAB-NaCMC (1 : 1) retarded drug release up to 96.7 ± 1.15%, while com- bination of CAB-MTH and MTH-NaCMC retarded drug release up to 81.9 ± 1.5% and 101.4 ± 1.3%, respec- tively, at the same polymer concentration. Core enteric coated tablet of ATVC (K 11) was compressed over with CLB and ASP granules with the help of CCT and produced the desired results with zero order release rate thus indicating successful formulation of proposed polypill.