Advanced Concepts in Pharmaceutical Research Vol. 7

Aneuploidy: Marker of Malignant Colorectal Adenomas

Stoian Marilena — Fri, 23 Feb 2024 00:00:00 +0000

Abnormal DNA amounts are mostly caused by changes in the number of chromosomes and chromosomal deletions. The aim of this study is to further investigate if DNA aneuploidy can serve as an early marker of malignant transformation of colorectal adenomatous polyps. The study was performed on 50 colorectal polyps obtained through endoscopic polypectomy from 46 patients, aged 30 to 80, with a mean age of 60. One interesting observation in our study refers to the DNA index in polyps with focal carcinomatous lesions, in which the carcinomatous areas have similar DNA indexes to those from the strictly adenomatous regions of the polyp. The significant association between DNA aneuploidy and the size of the polyps is vital, as size is considered one of the most important predictors of carcinomatous transformation in an adenoma, followed in predictive ability by histopathological type and degree of dysplasia.

Drug Repurposing of Pharmaceutical Products and Antimicrobial Discovery

Haripriya G. , Jatin Batra , Alan Joseph — Fri, 23 Feb 2024 00:00:00 +0000

The process of identifying new therapeutic uses for existing medications is known as drug repurposing. It's a good way to find or develop new drug compounds with different pharmacological applications. In recent years, numerous pharmaceutical companies have used the drug reformulation technique in their Research and Development of pharmaceuticals programmes to produce new medications based on the identification of new biological drug targets. This technique is extremely efficient, saves time, minimal cost, and has a low risk of failure. It boosts a drug's therapeutic value and its success rate. As a result, drug repositioning is a viable alternative to the standard drug development procedure. Identifying novel molecular compounds by de novo approach of drug is challenging, tedious and costly endeavor. To identify novel use of drug molecules many laboratory and drug interactions is been done. It is thus thought to be a developing method in existing drug, which have previously been shown safe in people and are in turn used to tackle rare and complicated diseases. Biopharmaceutical businesses have struggled to get the anticipated results when aiming to boost productivity through novel discovery technologies. Repositioning existing medications for new indications could help the industry achieve productivity gains. More firms are looking for repositioning options in their existing pharmacopoeia, and the number of drug repurposing has many success stories.

An Ethnomedicinal Study of Medicinal Plants in Gharsi Village, Solan, India

Hemraj Vashist , Diksha Sharma , Naresh Vashist, Shivani Dogra — Fri, 23 Feb 2024 00:00:00 +0000

Background: Gharsi village is a small village situated in the north-west of Solan district 50kilometer from Solan district at an elevation of 1300 meter from sea level. An exhaustive ethnomedicinal investigation of plants was carried out in Gharsi village and its allied valleys of Solan district.

Methods: The paper encompasses 60 medicinal plants. These plants were collected from the forest of Gharsi village and authenticated. This study is primarily concerned with the therapeutic properties of medicinal plants. The information was collected from local people and the list being mentioned is expected to prove helpful in short-listing the plant species found in this area.

Results: It was revealed that a total of 58 medicinal plants are very valuable medicinal plants and are already known for their numerous medicinal values.

Conclusion: This study will assist the forest, pharmaceutical firm, medicos, and wildlife manager in their efforts to improve the public health service and medicinal plant wealth of the area.

Ethnonutraceutical Resource Picrorhiza kurroa Royle ex. Benth: Strategic Approaches for Its Sustainable Management Toward Conservation and Healthcare Benefits

Fri, 23 Feb 2024 00:00:00 +0000

Picrorhiza kurroa, traditional Himalayan herb popularly known as kutki, had been emerged now as the most promising plant for National/ International trade commodity. Excessive usages of this particular herb in various formulations made it vulnerable. Thus, its propagation through micro/macro propagation methods for its further better conservation has been realized. Owing to its large demand in the local and global market for its established pharmaceuticals and nutraceuticals potential are well recognized at present. In view of the described fact, we access its availability from the grower’s field from mid Himalaya of Kumaun region of Uttarakhand (India). During rearing of accessed kutki plants from grower’s fields which were maintained at biotech product testing facilities (green house facilities) as well as under laboratory in vitro practices, these were nurtured and established in pots for further in vitro establishment. Thus, pot containing soil: sand: compost in the 1:1:1 ratio where field grown plants were nurtured and nourished. Powdery mildew caused by the fungus stressed these plants. However, this stress could be managed by foliar application of 0.2% (w/v) sulfur in water and 0.2% (v/v) mild (Tween-20) aqueous detergent solutions. Imidacloprid (0.2% v/v) was also required to spray to avoid sucking pests (Aphids and Thripes) infestations. The data of explants after control of infection and infestation and prior to control were compared. While establishing explants in vitro, our data showed better establishment on infection and infestation under control. However, molecular characterization for infection and infestation behavior yet is underway. Murashige and Skoog medium while supplemented with 0.5mg/L Thidiazuron (TDZ) and 0.5mg/L Indole butyric acid (IBA) based on our previous studies and checker board for identifying suitable concentrations of growth regulators, showedgood callus induction rate. Callus growth was maintained through subsequent sub-culturing based on callus growth conditions. It is worth mentioning that the use of soluble Polyvinylpyrrolidone (PVP) 0.03-0.05% w/v significantly removed phenolics exudates and sufficient for maintaining callus growth and viability. Beside, orientation of molecules is important to assess their promising biological activities. In view of this particular fact Fourier Transform Infrared (FTIR) analysis offering valuable insights for the molecules extracted from the induced callus for various functional groups. This will provide some understanding of bioactivities from this important ethnic plant resource too.

Recent Development and Validation of Tolperisone HCl and Diclofenac Sodium in Bulk and Pharmaceutical Dosage Forms by Using RP HPLC Method

M. Archana , M. Sumithra — Fri, 23 Feb 2024 00:00:00 +0000

High-performance liquid chromatography is at present one of the most sophisticated tools for analysis. The estimation of Tolperisone HCl and Diclofenac sodium was done by RP-HPLC. Tolperisone is an oral, centrally-acting muscle relaxant. The Phosphate buffer was p^H 3.0 and the mobile phase was optimized consisting of Methanol: Phosphate buffer mixed in the ratio of 70:30% v/ v. Inertsil C18 column C18 (4.6 x 150mm, 5\(\mu\)m) or equivalent chemically bonded to porous silica particles was used as stationary phase. The detection was carried out using a UV detector at 260 nm. The samples are weighed using the Afcoset ER-200A weighing balance. The solutions were chromatographed at a constant flow rate of 0.8 ml/min. the linearity range of Tolperisone HCl and Diclofenac sodium was found to be from 100-500 \(\mu\)g/ml of Tolperisone hcl and 1-5\(\mu\)g/ml of Diclofenac sodium. The linear regression coefficient was not more than 0. 999. The values of % RSD are less than 2% indicating the accuracy and precision of the method. The percentage recovery varies from 98-102% of Tolperisone HCl Diclofenac sodium. LOD and LOQ were found to be within the limit. The results obtained on the validation parameters met ICH and USP requirements.

Synthesis, Characterization, and Antioxidant Evaluation of Novel Ethoxylated Pyrazoline Derivatives: Promising Molecules for Drug Design in Pharmaceutical and Chemical Industries

B. Lakshminarayanan , Vijayakumar B. , P. Parthiban , N. Kannappan — Fri, 23 Feb 2024 00:00:00 +0000

Pyrazolines are the most important class of compounds in the pharmaceutical and chemical industries and (are considered) the most promising molecules for the design of new drugs. In this study, eleven novel ethoxylated pyrazoline derivatives were synthesized by condensing chalcones with an ethoxy group and hydrazine hydrate in the presence of alcohol, highlighting their significance as promising molecules for drug design in the pharmaceutical and chemical industries. The synthesized compounds underwent thorough characterization using ¹H NMR, ¹³C NMR, and mass spectra. Evaluation of these compounds for in vitro antioxidant activity through 2,2’-diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxide assay methods revealed moderate to good antioxidant properties. Notably, the compound EH2, with a methoxy group, displayed potent antioxidant activity with IC₅₀ values of 9.02 and 9.44µg/ml, while EH9, featuring a hydroxy group, exhibited significant antioxidant activity with IC₅₀ values of 12.41 and 14.56µg/ml in DPPH and hydrogen peroxide assays, respectively, surpassing the standard. Compounds containing electron-donating substituents demonstrated superior antioxidant capabilities compared to the standard ascorbic acid.

General Description of Pharmaceutical Tablet Punching Machine: An Overview

Sushma Desai, Jayapal Reddy Gangadi, Chandrasekhara Rao Baru — Fri, 23 Feb 2024 00:00:00 +0000

This study described a general description of pharmaceutical tablet punching machine. Making a pharmaceutical tablet is a challenging process. You must combine the active medicinal ingredient in the correct dosage with other necessary materials and press it into a tablet. A pharmaceutical tablet press machine does this process. Tablet press tool since its invention 19 century improving the efficiency of the basic model by studying various parameters, overcoming their problems and developing into a fully automated machine meeting the demands of high quality with low cost medicines production in time to ever-growing population, complying with cGMP (current good manufacturing practices) cleanliness standards, multiple ailments. Every pharmacy institution plans to have either of the tablets punching machine for sure. The tablets may be described as a compressed solid pharmaceutical unit dosage form. they stand unique among all the pharmaceutical formulations as a tamper proof preparation. Different manufacturers customize the amount of punches, stations, compression points, and speed of their tablet presses. Therefore, it is necessary to learn about pharmaceutical tablet punching machines, including how they operate and what kinds of tablets can be made using them using any one of the three recognized methods—direct compression, wet granulation, or compression granulation—or a combination of them. The common tableting process defects caused and to overcome these problems by the tablet press tooling and performance to be evaluated parameters are studied to estimate the working efficiency of the machine at every stage with the help of ISTMs (instrumented single tablet punching machine), IRTMs (instrumented rotary tablet punching machine) investigated with the achieved data is interpreted for selection of suitable tablet press to work on.

In-vivo Photothermal and Photodynamic Therapy for Tumors Using a Theranostic Strategy Based on Graphene Oxide

Fri, 23 Feb 2024 00:00:00 +0000

Cancer is the second leading cause of death globally and is responsible for about 1 in 6 deaths in the world. Therefore, there is a demand to introduce novel, effective antitumor agents delivered to their specific target tissue/site to improve the efficiency of cancer diagnosis and treatment and limit the undesired systemic adverse effects caused by conventional chemotherapeutic agents. In this context, graphene oxide (GO) has garnered interest in biomedicine for cancer therapy due to its distinct physical and chemical properties.

This study describes the in vivo application of Graphene Oxide (nc-GO) nanocomposites whose surfaces have been modified with PEG-folic acid, Rhodamine B, and Indocyanine Green. In addition to displaying red fluorescence spectra of Rhodamine B acting as the fluorescent marker, in vivo experiments were performed using nc-GO to apply Photodynamic Therapy and Photothermal Therapy in the treatment of Ehrlich tumors in mice using Near-Infrared Light (808 nm 1.8 W/cm2).

This study utilized fluorescence images to analyze the tumor, aiming to achieve the highest concentration of nc-GO over time (time after intraperitoneal injection). The resulting time data was then employed to optimize the tumor treatment through PDT / PTT. The current study shows an example of the successful use of nc-GO nanocomposites as a theranostic nanomedicine to perform simultaneously In vivo fluorescence diagnostics and combined PDT-PTT effects for cancer treatments.

GRAPHIC ABSTRACT

Fig. 1 shows a self-explanatory graphical summary of the present study.

Fig. 1. In vivo fluorescence spectra and treatment of tumor based on GO- nanocomposites

Bioanalytical Method Development and Validation of Garenoxacin Mesylate in Human Plasma by RP-HPLC and Its Pharmacokinetic Application

A. Ajitha, K. Sujatha — Fri, 23 Feb 2024 00:00:00 +0000

A simple, precise, accurate RP-HPLC method was developed for the estimation of Garenoxacin mesylate in human plasma using Ciprofloxacin Hydrochloride as an internal standard. The chromatographic conditions optimized were Zorbax Eclipse XDB C18 (250 x 4.6 mm, 5\(\mu\)) column, Mobile phase 0.1% OrthoPhosphoric Acid and Acetonitrile in the ratio of 50:50 (% v/v) with a flow rate of 1.0 ml/min and injection volume of 50 µL. The detection wavelength was set to 240 nm with a column temperature of 30^°C. The retention time of Garenoxacin mesylate was found to be 4.0 min. % Coefficient of Variation of Garenoxacin mesylate was found to be 4.30. % Recovery was obtained as 98.97%. The linearity of the proposed method was established in the concentration range of 0.04 to 4 µg/ml (Correlation Coefficient = 0.999). The lower limit of quantification was 0.04 µg/ml which reached the level of a drug possibly found in human plasma. Further, the reported method was validated as per the ICH guidelines and found to be well within the acceptable range. The method was successfully applied to a pharmacokinetic study after oral administration of immediate-release Zinox tablets (200 mg) in healthy Albino rabbits. The mean Cmax was found to be 5540 ng/ml, which occurred at a Tmax of 1.00 hr. The half-life and AUC0-\(\alpha\) values were found to be 13.52 hr and 72187 ng. hr/ml. The method was found to be applicable to bioequivalence studies.

In vitro Antibacterial Activity of Direct Crude Extracts of Carica papaya Leaves and Allium sativum Cloves Alone and in Combination against Multidrug Resistant Bacterial Strains

Srividya Lonkala, Prasadaswamy Thirunahari — Fri, 23 Feb 2024 00:00:00 +0000

Aim: Medicinal plants have potential pharmacological effect and Screening of natural extracts is a focused intensive study that aims to find active principles sorted from plant resources both safe and environmental friendly.

The present study was aimed to evaluate the antibacterial activity of direct crude extracts of Carica papaya leaves and Allium sativum cloves alone and in combination against multiple drug resistant strains.

Methods: The antibacterial potency of each plant extract individually and in combination was evaluated using five bacterial strains causing infections. Two Gram positive (Staphylococcus aureus and Bacillus cereus) and three strains of Gram negative (Escherichia coli, Salmonella typhi and Pseudomonas aeruginosa) bacteria were used to evaluate the antibacterial activity of Carica papaya leaves and Allium sativum using Agar Disk Diffusion Method.

Results: The results revealed that Carica papaya leaves extract and Allium sativum cloves extracts were potentially effective in suppressing microbial growth with variable potency. The combination of extracts of both plants was found to be most effective combination in retarding microbial growth of all tested pathogenic bacteria at concentration of 10 mg/disc than individual extracts.

Conclusion: The extracts have the potential to serve as natural alternatives for preventing food poisoning and preserving food while avoiding the potential health risks associated with the use of chemically antibacterial agents.