Advanced Concepts in Pharmaceutical Research Vol. 1

Objective: The aim of the present study was to design and evaluation of mouth dissolving oral films of tofacitinib citrate allowing fast reproducible drug dissolution in oral cavity thus bypassing the first-pass metabolism to enhance the patient convenience.

Method: Films has been prepared by solvent casting technique by using Polymer and Plasticizers.

Results: The results of prepared film pH, Thickness, Folding Endurance, Disintegration time, drug content was found in the suitable range.

Conclusion: The present study shown that the MDFs of Tofacitinib could be successfully prepared by solvent casting technique. Further, it was concluded that formulation F3 and F6 containing 45% w/w and 50% w/w of polymer concentration respectively were found to be having satisfactory physicochemical and mechanical properties. Also, the stability study of these two optimized formulations confirmed the longer shelf life of MDFs.

The objective of this study was to see how an ethanolic extract of Tecoma stans affected diabetic cardiomyopathy in wistar rats after streptozotocin-induced diabetes.  The pathogenesis of diabetic cardiomyopathy (DCM) is complex, and the therapeutic options available to treat DCM are limited. A single intravenous dosage of (Streptozotocin 45 mg/kg) produced diabetes in male wistar rats. Blood pressure, serum lactate dehydrogenase (LDH), glucose apolipoprotein B, and lipids were measured, as well as heart weight, caspase-3, sodium potassium adenosine triphosphatase (Na + -K + ATPase), and DNA laddering.  The obtained result showed that the administration of ethanolic extract of Tecoma stans (120 mg/kg/p.o.) significantly (P < 0.01) reduced myocyte loss by suppressing the levels of cardiac caspase-3, DNA laddering; mean arterial blood pressure and heart rate as well as serum LDH, glucose, apolipoprotein B and lipids levels. Further, it augmented the heart weight and cardiac Na+ K + ATPase activity in diabetic rats. Finally, an ethanol extract of Tecoma stans was found to have considerable anti-apoptotic potential in Streptozotocin-induced diabetic cardiomyopathy.

Cancer is a socially significant disease, since the incidence of oncological diseases is continuously growing worldwide. This necessitates the search for alternative therapeutic strategies beyond traditional chemo- and radiotherapy to reduce adverse effects, in particular high toxicity. Molecular chemotherapeutics have cytotoxic effects on both cancer cells and healthy dividing cells, in particular those of the immune system. The main problem of chemotherapy, selectivity, can be solved by using some distinctions of cancer cells from healthy cells. One such difference is their ability to phagocytose colloidal particles of submicron size. For this purpose, it is necessary to construct carrier particles through which molecular chemotherapeutics can be delivered and released inside the cancer cell.. Chemotherapeutic agents can be carried by nanoparticles, hydrogels, composed nanoparticle-hydrogels, micelles and liposomes. In this way, to achieve high transport efficiency, uptake and selectivity composite particles should be prepared starting from their physicochemical properties. The main focus of this book chapter is given to the surface properties as hydrophilicity/hydrophobicity and electric charge of nanoparticles formed from metal and dielectric substances: metals (gold, silver), metal-oxides of iron, aluminum, titanium and zirconium, silicates (quartz), alumosilicates (montmorillonite, kaolinite), and carbonates. The physicochemical properties of the nanoparticles are emphasized in order to assist researchers in choosing appropriate nanoparticles for adsorption of drugs with hydrophilic and hydrophobic organic molecules in order to synthesize composite particles for using as carriers of different anticancer agents.

The goal of this study is to create and test kanamycin for wound healing. Kanamycin is an antibiotic used as a first-line treatment. Kanamycin's absorption from the parentral pathway is improved by hydrogel. For the goal of wound healing, hydrogel outperforms traditional dose forms in terms of patient compliance. Carbomer (Carbopol) is utilized in the hydrogel formation. To improve the combining of the medication and the physical qualities of the hydrogel, five batches of hydrogel were made using varying concentrations of hydroxy propyl methyl cellulose and ethyl cellulose. The kanamycin is insoluble in PEG-400, but as per the procedure it is must to dissolve kanamycin in PEG-400. Therefore, a co-solvent study performed. Evaluation parameter such as appearance, solubility study, swelling measurement, spreadibility, percent drug entrapment efficiency, ph detection, and in-vitro release study were performed for hydrogels of each batch and batch- 3 was optimized best batch from all five batches. Batch-3 shows best solubility, swelling and percent drug entrapment properties. Batch-3 is able to release 91% drug release in 8 hr. The produced hydrogel shown good evaluation properties as well as storage stability. The hydrogel might be used as a medication delivery dosage form for a variety of reasons.

The objective of this study was to evaluate the impact of clinical pharmacist intervention on glycemic management using fasting blood glucose and glycosylated blood glucose levels.  Diabetes Mellitus is one of the world's fastest emerging chronic metabolic diseases which results in significantly raised morbidity, mortality, and healthcare expenses. The International Diabetes Foundation estimates diabetes in one in ten adults and about 47 % are under-diagnosed. Studies have shown that the risk factor for stroke and cardiovascular disease in diabetes patients is 2 to 3 times in contrast to patients having no hyperglycemia. A randomized prospective interventional study was conducted in the outpatient department of a tertiary care hospital. Patients suffering from diabetes for at least 2 years were selected for the study based on the inclusion and exclusion criteria. The control group was not given any special pharmacist care, while the interventional group had a face-to-face interview, counseling, and telephonic follow-up during the study period. Based on the baseline values and endpoint parametric values, the result of the study was analyzed. The study was analyzed based on the difference in the glycemic index, using HbA1c and FBS values. The basal values of HbA1c were similar for both groups (8.5%), but a marked reduction to 7.2% was observed in the interventional group. FBS values reduced from 208 mg/dl to 186 mg/dl in the intervention group, while in the usual care group, the reduction was from 211 mg/dl to 198 mg/dl.  HbA1c and fasting blood sugar significantly decreased as a result of the clinical pharmacist's intervention. For the purpose of maximizing pharmacotherapy, the clinical pharmacist participated in patient counseling and education throughout the trial. Through one-on-one meetings, material distribution, and telephone follow-up, it was accomplished. The patient now has a better understanding of how to change their lifestyle in addition to using their medications as prescribed. Through their interactions with the members of the intervention group, the usual care group also felt the effects of the research. Because of this, the standard care group also saw superior clinical results.

Pharmaceutical serialization is a legal requirement that ensures each unit of prescribed medication is given a special identification number. In the supply chain, this unique identification is utilized for product tracking and authentication. To reduce the risk of fake medications entering the US market, the Drug Supply Chain Security Act (DSCSA) first introduced pharmaceutical drug serialization laws in 2018. A 2D data matrix barcode encoded with a unique identity must be printed on each drug unit by the pharmaceutical drug maker. Basically, the risk of drug counterfeiting cannot be completely eliminated by simply printing a special identifying code for authenticity and traceability on each prescription medicines. Therefore, by copying the identical information in numerous units, criminals and drug counterfeiters can still introduce unlawful or stolen medications into the supply chain through an illicit source or online commerce. We discovered that the US market lacked a technology to authenticate individual medicine units with a centralized, secure repository before dispensing them to patients. The United States ultimately requires a integrated on-demand technology where all approved trading partners to be connected for drug authentication. Before releasing medicines into the market, the manufacturer must update the product's unique identifier in the centrally connected hub database. This procedure will guarantee that patients are receiving genuine medication and reduce the possibility of administering unauthorized or counterfeit pharmaceuticals.

Over the past few years, diagnosis and treatment of various diseases have become a significant challenge due to drug resistance, poor bioavailability, drug toxicity and high medication costs. Maximum drugs are hydrophobic in nature, and their efficacy depends on the route of administration. Hence, finding a new drug delivery system is essential for improving drug absorbability, pharmacokinetics, metabolism, metabolic effect duration, and minimizing toxicity. These days, the application of nanotechnology, such as nanoparticle nanomaterial, leaves a golden trail in the health sector. Nanomaterials differ from bulk materials of the same composition due to their distinctive physicochemical features, such as their small size, high surface area to mass ratio, and high reactivity. Nanoparticles (NPs) are divided into categories based on shape, size, nature, and composition like metallic nanoparticles (MNPs), porous nanoparticles, mesoporous nanoparticles, carbon nanotubes etc. Various metals and nonmetals, like silver, gold, silicon, and calcium phosphate, are used in nanoparticle preparation for anticancer, anti-microbial, bone regeneration etc. Not only the biomedical sector, metallic nanoparticle also has primary functions in textiles, the agriculture industry etc. The drawback of metallic nanoparticles is that they are prepared by toxic chemicals and require high energy. Some MNPs also posses has several toxicities. The alternative way to prepare metallic nanoparticles is using by plants, bacteria and fungi. Green synthesis is a promising way that allows low energy and low cost with less toxicity. This review gives an overview of metallic nanoparticles used in drug delivery systems.

The present research examined the antibacterial activity of nasal isolates on Buchholzia coriacea (Wonderful Kola) leaf extract. There is a lengthy history of traditional medicine. It is the whole of the knowledge, skill, and behaviors based on ideas, beliefs, and experiences that are inherent to many cultures, whether or not they can be explained, and employed in the preservation of health as well as in the avoidance, diagnosis, improvement, or treatment of physical and mental disease. One hundred pupils at the Delta State Polytechnic in Ogwash-uku, Delta State, were tested for nasal isolates. Using the agar well diffusion method, the antibacterial activity of the methanolic extract of the leaves was evaluated against nasally isolated microorganisms (E. coli, Citrobacter species, Klebsiella species, and Proteus species). Inhibition zones and Minimum Inhibitory Concentration (MIC) were used as indicators of antimicrobial activity. The extracts inhibited the growth of the bacterial isolates in a concentration dependent manner with MICs of 39.81mg/ml, 69.18mg/ml, 79.43mg/ml and 97.7mg/ml (E. coli, Citrobacter species, Klebsiella species and Proteus species) respectively. Phytochemical screening reveals the presence of secondary metabolites; tannins, saponins, cardiac glycosides, purines, reducing sugars, flavonoids, steroids, alkalloids and phlobatannins. The result indicates promising antibacterial potential of B. coriacea leaf extracts and hence could be considered for pharmaceutical and medicinal purposes. Characterization of the bioactive components of B. coriacea leaves could be used in the development of drugs for the treatment of bacterial related infections.

The goal of the study is to create metal complexes that are higher than schiff's base using metals like copper, metal, and metallic element, as well as to synthesis schiff's base, an antibacterial medication, using aromatic organic compounds like p-diethyl amino benzyldehyde and p-dimethyl amino benzyldehyde. Schiff bases are versatile organic compounds which are widely used and synthesized by condensation reaction of different amino compound with aldehydes or ketones known as imine. Schiff base ligands are considered as privileged ligands as they are simply synthesized by condensation. The synthesized schiff’s bases were regenerate to its ion Schiff bases by treating with methyl group halide. The ion Schiff bases were regenerate to metal complexes by treating with metals like CuCl2, ZnCl2 and CdCl2. All the synthesized compounds were characterised by Elemental analysis, IR and ¹H proton magnetic resonance.  Docking study was performed to know the interaction of binding sites with protein receptor using MAO-B enzymes (PDB ID: 2BK5) and COX-2 enzyme (PDB ID: 5IKR) by Virtual Screening software for Computational Drug Discovery. Synthesized metal complexes were evaluated for antibacterial, anti inflammatory and antidepressant activity. Copper metal complexes showed potent antibacterial and anti-inflammatory activity. Significant anti-depressant activity was shown for 2A2 and 2B2 zinc metal complexes.

Black beans (Phaseolus vulgaris L.) are most widely consumed in China, India, and America due to their unique taste and potent health benefits attributed to their higher content of phytochemicals. Researchers have extensively explored the phenolic profile and biological properties of black beans. Since ancient times, restorative spices have been discovered and used in traditional medical practices. The French bean, or Phaseolus vulgaris Linn. (Family: Fabaceae), is a carbohydrate and protein-rich food crop with healing properties that is extremely enticing. This plant contains a variety of nutrients, including carbohydrates, proteins, flavonoids, saponins, tannins, and phenolic acids.

The seeds of Phaseolus vulgaris Linn. have having Hostile to urolithiatic action and Against stoutness action. This survey gives a rundown of phytochemistry and pharmacological impact of Phaseolus vulgaris Linn., The plant can be additionally researched for other pharmacological exercises as it contains assortment of compound constituents and it is a generally utilizing food yield and clinical cures of this plant are sync with nature.

The idea of bio-enhancer originated from Ayurveda. Numerous methods exist to improve the bioavailability of drugs, with one of the latest being bioavailability enhancers. Herbal bio-enhancers improve bioavailability due to their absorption, safety, and minimal side effects. They increase drug bioavailability, which affects therapeutic efficacy, and when paired with appropriate drugs, enhance their effectiveness. This combination reduces drug dosage, cost, toxicity, side effects, and speeds up the drug's action. The survey aims to explore the concept of bioavailability in natural pharmaceuticals to achieve better therapeutic outcomes, as well as to classify bio-enhancers, understand their mechanism of action, evaluate commercial formulations, and assess future prospects.

In order to overcome the drawbacks of traditional topical formulation, the goal of this study is to design and characterize a salicylic acid film-forming gel of hydrophilic polymers for the treatment of hyperkeratotic and scaling disorders that has wipe-off resistance, longer retention at the treatment site, and is simple to spread and apply to the skin. Hyperkeratosis refers to the increased thickness of the stratum corneum, the outer layer of the skin. It is most frequently due to chronic physical or chemical damage such as friction or the use of aggressive soaps but can also derive from chronic inflammation or a side-effect of different drugs, including chemotherapy. Salicylic acid can be used topically to treat hyperkeratotic disorders, which are skin conditions characterized by red, dry, cracked, and scaling skin. The film-forming gel is prepared with HPMC E15, carbopol 934, propylene glycol, water, ethanol, and the drug. It is then optimised using 2² factorial designs and is characterised by its physical characteristics, pH level, spreadability, drug content, rheological study, in vitro drug release, drying time, mechanical properties of the film, and other factors. Salicylic acid film-forming gel stability, skin irritancy, ex vivo permeation, and skin retention were also investigated. For certain tests, every formulation produces the expected results. The optimisation analysis found that viscosity increases and drug release decreases when HPMC E15 and carbopol 934 concentrations rise. The improved formulation had a viscosity of 47.6 ± 1.23 cp and a 90.23 ± 2.01% drug release. It is concluded that salicylic acid film-forming gel for the treatment of hyperkeratotic and scaling diseases is efficiently produced with hydrophilic polymers i.e., HPMC E15 and Carbopol 934 and which has wipe off resistance, longer retention at the site of treatment, easy to spread on application and it forms a thin, transparent, protective, emollient and water soluble film on skin within few minutes to overcome the disadvantages of convention topical formulation like ointment, cream, gel i.e. need to rubbing, poor adherence to the skin, easily wiped off due to clothes, sweat, movements, poor permeability, compromised patient compliance.