Journal of Pharmaceutical Research Science & Technology [ ISSN: 2583-3332] <p><strong>Journal of Pharmaceutical Research Science &amp; Technology</strong> is an open access peer reviewed journal. It is permanently archived in<a href=""> Portico</a> (United Kingdom).</p> <p><em><strong>ISSN: 2583-3332</strong></em></p> en-US (Dr. MA Jahangir) (Dr. Sadaf Jamal Gilani) Mon, 07 Feb 2022 00:00:00 +0000 OJS 60 The Impact of Microsponge and Microsphere on Improving Oral Bioavailability of Medications: A Short Review <p><em>While many diseases require an efficient drug delivery technology that has the ability to improve bioavailability and alleviate side effects, various types of gastroretentive drug delivery systems (GRDDS) have been developed in order to overcome the obstacles, which are related to a narrow absorption window, instability, site of action, side effects, and dosing frequency. In this context, microsponge and microsphere systems depict two different types of GRDDS, aiming to provide adequate time for active ingredients to be absorbed in the stomach despite the variation in releasing mechanisms of the entrapped ingredients. For the successful designing of these systems, it is essential to optimize the characterizations of the formulated microparticles by considering physiological, pharmaceutical, and patient-related factors, which have a dramatic impact on the efficacy. Consequently, they will demonstrate different behaviors at the desired site of action, determining which systems are showing superiority compared to others. However, each microparticle system has some advantages over the others, providing more options for researchers to ease the difficulties that exist with conventional oral dosage forms. Therefore, this review aims to shed the light on critical factors that have significant impacts on microsponge and microsphere systems and addresses their advantages and disadvantages, providing an understanding of these criteria in order to optimize the drug systems.</em></p> Yasir Alshehry* and Mohammed Jafar Copyright (c) 2022 Yasir Alshehry* and Mohammed Jafar Mon, 07 Feb 2022 00:00:00 +0000 Oral Bioavailability Enhancement of Efavirenz using Piperine coadministration in Experimental Rabbits <p><strong><em>Background</em></strong><em>: Efavirenz, a first line anti-retroviral drug has variable bioavailability owing to its limited aqueous solubility. Piperine, a bioavailability enhancer has been often used to enhance the bioavailability of many drugs.</em></p> <p><strong><em>Objective</em></strong><em>: The present study was aimed to investigate the possibility of improving the bioavailability of efavirenz using piperine.</em></p> <p><strong><em>Methods</em></strong><em>: Two doses of efavirenz 9.33 mg/kg and 28 mg/kg which corresponded to 200 and 600 mg/kg of human dose were selected. Single oral dose of efavirenz and piperine co administration was given to rabbit and at fixed time interval drug blood concentration was estimated by HPLC. Pharmacokinetic parameters of efavirenz and piperine co administration were determined. </em></p> <p><strong><em>Results</em></strong><em>: Efavirenz 9.33 mg/kg co administration with piperine 20.8 mg/kg increased area under the curve significantly at p&lt;0.01 and C<sub>max</sub> at p&lt;0.05 compared to efavirenz control (9.33 mg/kg). The relative bioavailability of efavirenz and piperine co-administration was found to be 149.08%, i.e., higher than efavirenz control. &nbsp;T<sub>1/2 </sub>of piperine co-administration was also increased significantly at p&lt;0.05 compared to efavirenz control. T<sub>max</sub> of piperine co-administration was found to be 0.5 h, followed by efavirenz control i.e., 1 h. Co-administration of efavirenz (28 mg/kg) with piperine (20.8 significantly increased AUC and C<sub>max</sub> at p&lt;0.001 compared to efavirenz control (28 mg/kg). The relative bioavailability of Piperine co-administration was found to be 158.92%, higher than efavirenz control. There was significant increase in T<sub>1/2 </sub>of piperine co-administration at p&lt;0.01 compared to efavirenz control. T<sub>max</sub> of piperine co-administration and efavirenz were found to be same i.e., 1 h.</em></p> <p><strong><em>Conclusion</em></strong><em>: Based on the results it can be concluded that piperine co-administration significantly increases the oral exposure of efavirenz. Bioavailability of efavirenz with piperine was found to be higher than efavirenz control.</em></p> Mohammad Asif *, Hardik P Patel and Rakesh K Patel Copyright (c) 2022 Mohammad Asif *, Hardik P Patel and Rakesh K Patel Mon, 07 Feb 2022 00:00:00 +0000 Evaluation of Antioxidant Activity of Obtained Derivatives of Vanillin <p><strong><em>Background</em></strong><em>: Vanillin is a white monoclinic crystalline compound whose chemical nomenclature is p-hydroxy-m-methoxy benzaldehyde. It is a phenolic aldehyde with a pleasant flavor and popularly found in vanilla beans and roasted coffee amongst many other sources. It serves as in addition; it possesses antitumor and particularly antioxidant activity which formed the essence of this study.&nbsp; </em></p> <p><strong><em>Objectives</em></strong><em>: The insidious presence of free oxygenated and nitrogen radicals in the human body has become a worrisome concern. These chemical species continue to plague the human cells, tissues and organs resulting in different pathophysiological conditions such as cancers and neurodegenerative disorders like Alzheimer’s disease and Parkinson’s disease amongst many other ailments. The search for novel pharmacological compounds with the aim of curbing the rising incidence of these radicals led the choice of vanillin in this present study.&nbsp;&nbsp; </em></p> <p><strong><em>Methodology</em></strong><em>: Vanillin was separately subjected to a series of derivatization reactions namely, acetylation, O-demethylation, reduction and oxidation. The melting points, refractive indices and optical rotations of the lead compound and derivatives were obtained. The antioxidant activities of the five compounds were determined using the DPPH (2, 2-diphenyl-1-picrylhydrazyl hydrate) test. Comparison of the obtained antioxidant activities was done to determine if any improvements could be seen in the derivatives.&nbsp;&nbsp;&nbsp; </em></p> <p><strong><em>Results</em></strong><em>: The identities of the derivatives have been revealed to be vanillyl acetate (E-1) (acetyl derivative), 3, 4-dihydroxy benzaldehyde or protocatechui aldehyde (E-2) (demethylated derivative), o-methoxy-p-methyl cyclohexan-1-ol (J-1) (reduced derivative) and vanillic acid </em></p> <p><em>(J-2) (oxidized derivative) respectively using the IR spectral technique. Vanillin, E-2 and J-2 derivatives gave marginal antioxidant activity of IC50 of 0.81, 0.84 and 0.0.85 µg/mL respectively while J-1 and E-1 demonstrated moderately significant IC50 of 0.59 and 0.63 µg/mL which compare favorably with 0.44 µg/mL elicited by Vitamin C (a standard antioxidant drug). It is pertinent to point out that the obtained reduced derivative is a substituted cycloalkanol (a saturated cyclic compound) instead of a substituted phenolic compound as was expected.</em></p> <p><strong><em>Conclusion</em></strong><em>: The results from this study indicate that reduction and acetylation separately enhance the antioxidant activity of vanillin.</em></p> Olawale Hakeem Oladimeji*, Stanllinus Njinga, and Saad Toyin Abdullahi Copyright (c) 2022 Olawale Hakeem Oladimeji*, Ekemini Samuel Idiong, Udeme Akpan Joseph, Victor Udo Anah, Moji Taibat Bakare-Odunola, Stanllinus Njinga, and Saad Toyin Abdullahi Mon, 07 Feb 2022 00:00:00 +0000 Nanophytomedicine in clinical management: An introductory evidence-based review <p><strong>Introduction:</strong> Herbal medicines are an important ingredient of traditional and alternative medicinal system and thus being used since ancient times. Owing to their characteristic of having lesser side effects and potential therapeutic effect they have drawn attention of pharmaceutical scientists from across the globe. Herbal medicines have now strongly captured a whooping US $62 billion market globally. Herbal medicines have been widely accepted of their potential to treat chronic diseases, low toxicity profile, cheap and wide availability etc.</p> <p><strong>Methods:</strong> The Safety and efficacy of herbal drugs have played an important part in their successful commercialization. With the emergence and application of nanotechnology the bioavailability and bioactivity of herbal medicines have improved drastically.</p> <p><strong>Results:</strong> Development of nano-phytomedicines by reducing their size to nano scale range, attaching it with polymers and by modifying their surface properties, solubility, permeability, eventually enhances the bioavailability of herbal formulations.</p> <p><strong>Conclusion:</strong> Novel formulations like niosomes, liposomes, nanospheres, phytosomes etc. can be exploited in this area. However, novel nano-phytomedicinescomes with its own pros and cons. This article extensively reviews herbal nano-medicines with its reported success and failures.</p> Mohammed Asadullah Jahangir, Sumayya Khan, Anirudh Dev Singh, Abdul Muheem, Arti Soni and Mohamad Taleuzzaman* Copyright (c) 2022 Mohammed Asadullah Jahangir, Sumayya Khan, Anirudh Dev Singh, Abdul Muheem, Arti Soni, Mohamad Taleuzzaman Mon, 07 Feb 2022 00:00:00 +0000 Phytonutrients and Technological Development in Formulations <p><em>Phytomedicines are used by humans since ancient civilizations and is now considered as an important part of traditional and alternative system of medicine. In recent time, phytomedicines have gained special attention based on the fact that a number of current medicines are derived from plant source. Phytochemicals exhibits lesser side effects and are potentially strong therapeutic agents. The global market for herbal drugs is increasing day by day. It has gained widespread acceptance due to its efficacy, accessibility, minimum toxicity, and cost effectiveness. However, solubility, stability and bioavailability are some of the major hindrances in the commercialization process of phytomedicines. Nanotechnology have been potentially productive in improving the solubility, stability, bioavailability, and bioactivity of phytomedicines. Development of nano-phytomedicines or attaching phytomedicines with polymers and modifying their surface properties and permeability have altogether influenced the bioavailability of phytochemicals. Novel formulations like solid lipid nanoparticles, micelles, niosomes, dendrimers, nanotube, liposomes, nano-emulsions nanospheres, phytosomes etc. Have been developed loaded with phytomedicines and have shown extraordinary result. This chapter extensively reviews phytomedicines based novel drug delivery systems having potential activity in different diseases like metabolic disorders, cardiovascular disorders, neurological disorders, viral diseases, cancers, inflammatory diseases and wound healing and lastly future prospect is discussed.</em></p> Mohammed Asadullah Jahangir*, Ameeduzzafar Zafar, Sumayya Khan, Chandra Kala, Abdul Muheem, and Mohamad Taleuzzaman Copyright (c) 2022 Mohammed Asadullah Jahangir*, Ameeduzzafar Zafar, Sumayya Khan, Chandra Kala, Abdul Muheem, and Mohamad Taleuzzaman Mon, 07 Feb 2022 00:00:00 +0000 Stability of Binary Mixtures of Drugs at Different Concentrations and Temperatures <p><strong><em>Background and Objective</em></strong><em>: In order to avoid separate injections, admixtures of drugs are frequently used in palliative care setting. The objective of this work is to study the stability of binary mixtures of drugs (ondansetron and midazolam) at different concentrations and temperatures all prepared in 0.9% NaCl and stored into infusers and glass in all cases protected from light. </em></p> <p><strong><em>Materials and Methods</em></strong><em>: Two methods have been employed to determine periodically the concentration of each drug in the mixtures (HPLC-UV and UV-vis spectrophotometry methods). The concentrations of the samples were: 0.1 mg mL<sup>-1</sup> – 0.1 mg mL<sup>-1</sup> and 0.5 mg mL<sup>-1</sup> – 1.0 mg mL<sup>-1</sup> of ondansetron and midazolam respectively; temperature of storage 25ºC and 37ºC.&nbsp; NaCl 0.9% was used as diluent in all cases. The containers to store each mixture were three infusers and glass. </em></p> <p><strong><em>Results</em></strong><em>: All solutions were initially clear and colourless but visible particles appear, in all cases, into the infusers after two days since their preparation. </em></p> <p><strong><em>Conclusions</em></strong><em>: The admixture of ondansetron and midazolam in NaCl 0.9% is recommended to use for a maximum of one day, at the concentrations evaluated, over time it tends to precipitate. Infuser conditioning decreases stability with respect to other conditions materials, so other stability studies may not be extrapolated if stored under different conditions.</em></p> Espinosa-Bosch María, Sánchez-Rojas Fuensanta, and Bosch-Ojeda Catalina Copyright (c) 2022 Espinosa-Bosch María, Sánchez-Rojas Fuensanta, and Bosch-Ojeda Catalina Fri, 04 Mar 2022 00:00:00 +0000 Antibacterial Activity of Cassia abbreviata Oliv Bark Extract against Escherichia coli and Staphylococcus aureus <p><strong><em>Background</em></strong><em>: Cassia abbreviata Oliv is believed to possess many pharmacological activities and has been used traditionally to treat many ailments. In Zambia, it is used by traditional healers and the locals to treat various bacterial infections especially in rural areas where traditional medicine is the first or only line of treatment. However, it’s phytochemical content and activity on Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) has not been documented in Zambia. </em></p> <p><strong><em>Objective</em></strong><em>: To investigate the phytochemical composition and antibacterial activity of Cassia abbreviata Oliv stem bark extract against Escherichia coli and Staphylococcus aureus.</em></p> <p><strong><em>Materials and Methods</em></strong><em>: Ethanol and aqueous crude extracts were derived from Cassia abbreviata Oliv stem bark and subjected to qualitative phytochemical screening using standard procedures. The extracts were then used to test for antibacterial activity against standard cultures of E. coli ATCC 25922 and S. ATCC 25923. Ciprofloxacin (5µg) was used as a positive control. The agar disc diffusion was used to determine the antibacterial activity of C. abbreviata at different concentrations (20, 15, 10, 5 and 1mg/mL). The minimum inhibitory concentration (MIC) and zones of inhibition were measured against the tested microorganisms.</em></p> <p><strong><em>Results</em></strong><em>: The phytochemical screening revealed the presence of alkaloids, tannins, flavonoids, saponins, terpenoids, sterols, and phenols. The ethanolic extract was found to have antibacterial activity against S. aureus but not E. coli, while the aqueous extract had no effect on either pathogen. A minimum inhibitory concentration of 5mg/mL was observed with the ethanolic extract. Ciprofloxacin showed better antibacterial activity against both S. aureus and E. coli compared to the extracts. </em></p> <p><strong><em>Conclusion</em></strong><em>: The ethanolic extract showed a concentration-dependent antibacterial activity against S. aureus while the aqueous extract showed no antibacterial activity.</em></p> Christabel Nang’andu Hikaambo, Tumbila Chisanga, Martin Kampamba, Tumelo Muyenga Akapelwa, Tadious Chimombe, Martha Chulu, Namuchindo Nanyangwe, Reagan Kabuka and Steward Mudenda Copyright (c) 2022 Christabel Nang’andu Hikaambo, Tumbila Chisanga, Martin Kampamba, Tumelo Muyenga Akapelwa, Tadious Chimombe, Martha Chulu, Namuchindo Nanyangwe, Reagan Kabuka and Steward Mudenda Fri, 04 Mar 2022 00:00:00 +0000 Formulation and Evaluation of Combined Dosage Form of Diclofenac Sodium (Mini Tablet) and Omeprazole Sodium in Capsule Devices <p><em>The work investigates the formulation and evaluation of combined dosage form of diclofenac sodium (mini tablet) and omeprazole sodium in capsule devices. The design of effective and safe drug delivery systems has become an integral part for the development and formulating of new medicines. So, research continuously keeps on searching for new ways to deliver drugs over a long period of time or for a well-controlled release profile, to minimizing the loss of drug, to reduce the side effect. The continuous release mini matrix tablet of diclofenac sodium prepared by wet granulation using HPMC, the patients at risk for ulcer disease who require treatment for arthritis receive nonsteroidal anti-inflammatory drugs (NSAIDs) that are selective for cyclooxygenase-2 or the combination of a nonselective NSAID with a proton-pump inhibitor. We assessed whether celecoxib would be similar to diclofenac plus omeprazole in reducing the risk of recurrent ulcer bleeding in patients at high risk for bleeding.</em></p> Gangwar Sanni and Kumar Santosh Copyright (c) 2022 Gangwar Sanni and Kumar Santosh Fri, 04 Mar 2022 00:00:00 +0000