Ashu Mittal

This study aims to evaluate HM (high methoxyl) pectin from different sources (apple, citrus, and beet) with varying degrees of methyl esterification (DOE) to identify the optimal grade for colonic bacterial enzyme-triggered polymeric coatings for colon-targeted delivery of drugs. Drug-loaded multiparticulates were prepared by a powder layering technique and subsequently coated into distinct trial formulation batches with ethyl cellulose and different HM pectin-based plasticized coating solutions. Otilonium bromide, a model drug for irritable bowel syndrome, was employed. Drug-polymer compatibility was confirmed through FT-IR and DSC studies. The coated multiparticulates demonstrated high drug entrapment efficiency (>85%), favorable micromeritic properties, and minimal loose surface drug crystals (48 (p = 0.0042), coated with apple pectin (DOE 50%), exhibited superior colon-targeting efficiency, limiting drug release to 15.47 ± 1.53% under simulated upper gastrointestinal conditions while achieving 78.27 ± 2.11% release under colonic conditions by the ninth hour in vitro. Surface topography was analyzed via scanning electron microscopy before and after dissolution. In vivo, X-ray roentgenography, and gamma-scintigraphy studies in New Zealand white rabbits further validated the colon-targeting efficacy of the optimized batch. The source and DOE value of the HM pectin were found to affect premature drug release and colon-targeting efficiency. Apple HM pectin 50% DOE was found to be the ideal HM pectin for microbial enzyme-dependent colon-targeted coatings.

In this study, we aimed to prepare, evaluate, and compare drug-loaded pellets of ketoprofen coated with different triggering mechanisms for colonic delivery. The purpose of this study was to compare Eudragit S100 and Eudragit L100 based pH-dependent, hydroxypropyl cellulose and ethyl cellulose-based time-dependent and high methoxylated pectin and ethyl cellulose-based colonic bacterial enzymatic degradation-dependent coatings over drug-loaded pellets for most efficient colon targeting. Any possible drug-polymer interactions were analyzed using Fourier-transform infrared spectroscopy and differential scanning calorimetry. Drug-loaded pellets were prepared using powder layering technology. Different batches of coated pellets were prepared for in vitro evaluation, and optimized batches were selected. These optimized batches were investigated for surface topography by scanning electron microscopy and for colon targeting efficiency by in vivo X-ray roentgenography and gamma scintigraphy studies in white New Zealand rabbits. The drug and polymers were found to be compatible. The prepared coated multi-particulates exhibited favorable micrometric properties. In vitro dissolution studies showed that the polysaccharide pectin high methoxylated and ethyl cellulose-coated optimized batch limited drug release to 16.724 ± 1.124% in the upper gastrointestinal tract and released up to 91.556 ± 3.144% in the colon following zero-order Korsmeyer-peppas super case-II transport (mean dissolution time 36.1779 h). Scanning electron microscopy analysis confirmed the surface characteristics of the pellets before and after dissolution. In vivo studies in New Zealand white rabbits using X-ray roentgenography and gamma scintigraphy demonstrated the optimized batch's gastrointestinal transit and colon targeting efficiency. Statistically, the polysaccharide-based formulation showed promising results for targeted drug release in the colon.

Drug administration at similar doses in patients can often lead to various clinical responses. It has been hypothesized that genetics primarily accounts for variation in drug efficacy and toxicity in individuals. Personalized medicine has been a breakthrough achieved by the Human Genome Project which contributes to enhancing quality-based patient care. It deals with the customization of medication considering the distinct genetic and proteomic data that underpins the originality of every patient and every instance of therapeutic intervention. Many cases have shown that inter-individual differences related to drug response can be traced to genetic polymorphism in the gene alleles that codes for metabolizing enzymes, drug transporters, and genetic variations in a person’s Major Histocompatibility Complex (MHC). So, the paper throws an insight into epidemiological variations due to genetics, variations in response based on metabolic parameters, and transporters. It also covers genetic variation related to immune-related drug toxicities. Pharmacogenetic testing plays an important role in achieving more precise personalized therapeutics for better public health. The paper discusses various tests for human leukocyte antigen variants and metabolic variants. Every technology inclusion comes with advantages and limitations so personalized medicine also faces certain challenges which are discussed in the paper. Once personalized medicine is used in clinical settings, patients will be able to receive the best medications for them based on their unique genetic and protein profiles.

Background: Brexpiprazole (BRZ) is a "third-generation" antipsychotic dopaminergic (D2) and 5HT1A (serotonin) partial agonist, approved in July 2015 by the US Food and Drug Administration for the treatment of the major depressive disorder (MDD) other than schizophrenia in adults. Antipsychotics are known to produce extrapyramidal effects as side effects. The recent development in this segment is of piperazine-based antipsychotic BRZ, which is more specific towards indented indications (depression) and has fewer side effects. Objective: To critically review the different analytical methods available in the literature. Methods: Eight spectrophotometry-based studies, nineteen chromatography-based studies, and two other method-based studies were found in the literature search. A brief discussion on pharmacokinetics and the mechanism of action is also included. Conclutions: This review can be used for the development of more robust and suitable analytical methods for the determination of drugs in different matrices. A brief discussion concerning the approach towards the advancement of green analytical methods is likewise one of the points of this review.

Drug information centre refer to facility specially set aside for, and specializing in the provision of drug information and related issues. The purpose of drug information center is to provide authentic individualized, accurate, relevant and unbiased drug information to the consumers and healthcare professionals regarding medication related inquiries to the nation for health care and drug safety aspects by answering their call regarding the all critical problems on drug information, their uses and their side effects. Apart from that the center also provides in-depth, impartial source of crucial drug information to meet the needs of the practicing physicians, pharmacists and other health care professionals to safeguard the health, financial and legal interests of the patient and to broaden the pharmacist role visible in the society and community. The service should include collecting, reviewing, evaluating, indexing and distributing information on drugs to health workers. Drug and poisons information centers are best established within major teaching hospitals. This allows access to clinical experience, libraries, research facilities and educational activities. Information present in the current paper will not only enlighten the role of drug information center but also focused on the rational use of drug.

A simple, selective, rapid, and economical reversed phase high performance liquid chromatography(RP-HPLC) method for the determination of doxofylline in the commercial dosage form has been developed and validated. The separation and quantification were achieved on an HiQ Sil C 18 W column using a mobile phase of acetonitrile: buffer (50: 50), pH 3, at a flow rate of 1 mL/min with detection of analyte at 272 nm. The separation was achieved within 3.1 ± 0.3 min for doxofylline sample. The method showed good linearity in the range of 10–80 μg/mL. The intra and inter day RSD ranged from 0.37–0.53%. The recovery (mean ± S.D.) of low, middle and high concentrations were 100.04 ± 0.80, 100.01 ± 0.20, 100.07 ± 0.30 respectively. Limit of detection and limit of quantification were 0.03 and 0.1 μg/mL, respectively.

Objective: The main objective of the present study was to establish and evaluate matrix type transdermal therapeutic systems containing new polymeric combinations (Eudragit E PO/Eudragit RL 100 & Plasdone S 630) as polymers and Labetalol Hydrochloride (LBHCl) as a model drug. Experimental: The matrix type TTS of LBHCl were prepared by film casting technique. The patches were characterized for physical, in vitro release studies and ex-vivo permeation studies using human cadaver skin. On the basis of in vitro drug release study and skin permeation, formulation A1 was found more effective than the other formulations, so it was selected as the optimized formulation. The optimized formulation patch was assessed in detail for its pharmacokinetic, pharmacodynamic, skin irritation potential, and stability studies. Results: The maximum percentage drug release and Permeation in 48 hrs were 92.43 % and 76.24 % respectively for optimized patch. The Korsmeyer peppas release exponent value of 0.604 in the optimized formulation was highly suggestive of release mechanism towards first order release. The observations obtained from the in vivo characterization of the optimized patch were indicative of sustained action of the developed formulation. The interaction studies analysis indicated no chemical interaction among the drug and polymers. The optimized patch appeared free from potentially hazardous skin irritation as observed by skin irritation score of 0.915 < 2.00 (under Draize score test). The optimized formulation was found to be stable at ambient storage conditions. Conclusion: The above TTS holds promise for improved bioavailability and better management of hypertension in long term basis.

In the present study, we attempted to prepare biodegradable microspheres of polylactic acid containing aripiprazole in order to achieve its controlled release profile suitable for parenteral administration. Biodegradable microspheres were prepared by solvent evaporation method using methylene dichloride as a solvent. The optimization of various formulation variables (e.g., stirring speed, and polymer:drug ratio, stabilizer concentration) to obtain spherical particles was also investigated. The optimized product was further characterized for various in vitro attributes, such as particle size and its distribution, encapsulation efficiency, surface properties, percentage yield, and in vitro release. Changing the ratio of polymer, stabilizers, and leaching agent (sodium chloride) affected the entrapment efficiency and release rate of aripiprazole. The release quantum was 88.41% when stirring rate was 2000 rpm and it was further increased to 94.65% when stirring speed was increased to 3000 rpm (Formulation E). Drug entrapment of microspheres was increased by increasing the concentration of PVP and maximum entrapment (62.35%) was obtained at 4% concentration of PVP (Formulation E). Spherical particles with good surface characteristics were obtained at stirring rate 3000 rpm and drug:polymer ratio 1:10.