Design, Formulation and Physicochemical Evaluation of Clotrimazole Chewing Gum

Background: Oral candidiasis is widespread in the patients with immunodeficiency diseases. Chewing gums are considered as mobile drug delivery systems that affected locally or systemically via the oral cavity. This study aimed to develop and evaluate the formulation of clotrimazole chewing gums for patients having oral candidiasis. Materials and Methods: Fourteen formulations (F) were designed by Design-Expert, version 7. These formulations were different in the amount of gum bases and sweeteners. Gum bases of elvasti, 487, stick, and fruit C were heated up to 70°C. Clotrimazole powder, sugar, liquid glucose, glycerin, mannitol, xylitol, and maltitol as well as different flavoring agents were added to the gum bases at 40°C. Content and weight uniformity, organoleptic properties evaluation, releasing the active ingredient in the phosphate buffer pH, 6.8, and taste evaluation were analyzed by Latin square analysis. Also, the mechanical test was done on F13 and F14 formulations. Results: F14 was the best formulation in terms of organoleptic properties. This formulation had suitable size, hardness, softness, and lack of adhesion to teeth. F14 formulation released 89% and 97% of clotrimazole after 30 and 45 minutes, respectively. F14 content uniformity and weight variations were 9.83±0.086 mg and 1.14±0.09 g, respectively. F14 evaluation of mechanical properties showed Young’s modulus about 0.32 MPa, and yield point occurred at the stress of 0.599 MPa and strain of 4.1%. Conclusion: F14 was chosen according to its physicochemical and organoleptic properties. F14 had adequate hardness, lack of adhesion to the teeth, suitable size, and best drug release. Tutti Frutti was a proper flavoring agent for clotrimazole gum formulations.[GMJ.2021;10:e1084]

Formulation and Evaluation of Orodispersible Tablet of poorly water Soluble Drug ‘Fenofibrate’ by Using Solubility Enhancement Technique

In the recent years scientific and technological advancements have been made in the research and development of oral drug delivery systems. The aim of this study was to formulate and evaluate of orodispersible tablets by direct compression for fenofibrate by using super fast disintegrating agents like croscarmellose sodium. The use of super disintegrant and excipient for preparation of fast disintegrating is highly effective and commercially feasible. In the present investigation poorly water soluble drug is one of the most important parameters of oral formulations sucessfully developed fenofibrate was using solvent evaporation method drug: PEG 6000 in (1:5 w/w). The formulation F7 was the optimized formula that showed satisfactory results with various physicochemical evaluation parameters like thickness, hardness, weight variation, friability, drug content, % drug release almost 79.98% within 15 min. and it was follow the maximum higuchi release kinetics that regression coefficient values ‘r2’= 0.995.

In Vitro Biopharmaceutical and Physicochemical Evaluation of Different Brands of Ciprofloxacin Marketed in Aden-Yemen

The current study conducted to evaluate the biopharmaceutical and physicochemical equivalence of the three available pharmaceutical dosage forms of ciprofloxacin (CIP) in the local markets (tablets, infusion and eye drops). Three brands for each dosage form were selected and coded as Tablets I, II, III; CIP infusion (Infusion I, II, III) and CIP eye drops (Eye drops I, II, III). Different in vitro quality control tests, physiochemical and determination of active ingredients contents were performed. All brands of tablets have a satisfactory result that complies with the pharmacopeia specification except the hardness of the tablets was more than the recommended value, and the salinity of Infusion II and III was lower than 0.9, the viscosity of the eye drops was lower than the specified value. Post-marketing surveillance is an essential issue to distinguish poor-quality medicines and must be routinely performed to weed out substandard and counterfeit medicine.

Physicochemical Evaluation of Diploknema butyracea Seed Extract and Formulation of Ketoconazole Ointment by Using the Fat as a Base

The fat obtained from the ripened seeds of Diploknema butyracea is widely used as a vegetable oil in rural areas of Nepal. This study was aimed for the physicochemical evaluation (acid value, iodine value, saponification value, peroxide value, ester value, pH, and liquefaction point) of the Diploknema butyracea seed extract (chyuri fat) and the formulation of 2% w/w ketoconazole ointment by using it as a base. All the physicochemical parameters were determined quantitatively by using the method of Indian Pharmacopoeia (IP), volume-I. By fusion method, 3 different formulations F-A, F-B, and F-C were prepared, in which different proportions of chyuri fat, polyethylene glycol 6000 (PEG 600), Tween 80, and propylene glycol were used as an ointment base. Various quality parameters such as spreadability, extrudability, viscosity, smoothness, pH, average fill weight, assay, content uniformity, accelerated stability, and drug release profiles were determined. HPLC was used for the determination of ketoconazole content in the ointment formulations. Physicochemical evaluation of the chyuri fat ensured its suitability for industrial purpose. The active ingredient release profile of formulations F-A (87.71%), F-B (88.89%), and F-C (91.09%) after 5 hours were within acceptable range along with other parameters. Assay of the formulations F-A, F-B, and F-C were reported to be 103.01, 107.9, and 102.45%, respectively. Overall, evaluation of the formulation F-A, prepared by using chyrui fat only, gave satisfactory results and most of the parameters were statistically similar ( p > 0.05 ) to the F-B and F-C formulated by incorporating a certain proportion of synthetic base. Thus it can be concluded that chyuri fat can be the best alternative to replace the expensive synthetic base.

Formulation and evaluation of dry herbal powder shampoo

Shampoos are used not only for cleansing purpose but also for imparting gloss to hair and to maintain their manageability and oiliness for hair. Shampoos are of various types, like powder shampoo, clear liquid shampoo liquid shampoo, lotion shampoo, solid gel shampoo, medicated shampoo, liquid herbal shampoo etc. As far as herbal shampoos are concerned in stability criteria. Depending upon the nature of the ingredients they may be simple or plain shampoo, antiseptic or antidandruff.In the present work the herbal shampoo powder has been developed, by using traditional drugs for hair care. The preparation were formulated using Onion Powder, Rose Petal, Lemon Grass, Flaxseed or Linseed, Hirda, Bahera, Black tea, Brahmni, Triphala, Bhringraj, Ginger Root, Ashwagadha, Shikakai, Feenu greek, Shatavari, Heena, Wala, Aloevera Powder, Nirgudi Powder, Bavachi, Jatha mansi, Tulsi, Neem, Hibiscus Flower, and Retha evaluated for organoleptic properties, powder characteristics, foam test and physical evaluation.The physicochemical evaluation of the formulated shampoo showed ideal results. However, to improve its quality, product performance, and safety, further development and study was required.

Identifying the Most Potent Dual-Targeting Compound(s) against 3CLprotease and NSP15exonuclease of SARS-CoV-2 from Nigella sativa: Virtual Screening via Physicochemical Properties, Docking and Dynamic Simulation Analysis

Background: The outbreak of the coronavirus (SARS-CoV-2) has drastically affected the human population and caused enormous economic deprivation. It belongs to the β-coronavirus family and causes various problems such as acute respiratory distress syndrome and has resulted in a global pandemic. Though various medications have been under trial for combating COVID-19, specific medicine for treating COVID-19 is unavailable. Thus, the current situation urgently requires effective treatment modalities. Nigella sativa, a natural herb with reported antiviral activity and various pharmacological properties, has been selected in the present study to identify a therapeutic possibility for treating COVID-19. Methods: The present work aimed to virtually screen the bioactive compounds of N. sativa based on the physicochemical properties and docking approach against two SARS-CoV-2 enzymes responsible for crucial functions: 3CLpro (Main protease) and NSP15 (Nonstructural protein 15 or exonuclease). However, simulation trajectory analyses for 100ns were accomplished by using the YASARA STRUCTURE tool based on the AMBER14 force field with 400 snapshots every 250ps. RMSD and RMSF plots were successfully obtained for each target. Results: The results of molecular docking have shown higher binding energy of dithymoquinone (DTQ), a compound of N. sativa against 3CLpro and Nsp15, i.e., −8.56 kcal/mol and −8.31 kcal/mol, respectively. Further, the dynamic simulation has shown good stability of DTQ against both the targeted enzymes. In addition, physicochemical evaluation and toxicity assessment also revealed that DTQ obeyed the Lipinski rule and did not have any toxic side effects. Importantly, DTQ was much better in every aspect among the 13 N. sativa compounds and 2 control compounds tested. Conclusions: The results predicted that DTQ is a potent therapeutic molecule that could dual-target both 3CLpro and NSP15 for anti-COVID therapy.

Catalytic and Physicochemical Evaluation of a TiO2/ZnO/Laccase Biocatalytic System: Application in the Decolorization of Azo and Anthraquinone Dyes

A TiO2/ZnO oxide system was proposed as a support for the immobilization of laccase from Trametes versicolor (LTV). The obtained TiO2/ZnO/LTV biocatalytic system was then applied in the decolorization/degradation of C.I. Reactive Black 5 and C.I. Acid Green 25 dyes. The efficiency of immobilization was evaluated based on catalytic properties (Bradford method, oxidation reaction of 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) and physicochemical (spectroscopic, porous, electrokinetic) analysis. The immobilization process was carried out with high performance (99.4%). Immobilized laccase retained about 40% of its activity in the whole analyzed temperature range and after 10 reaction cycles. Immobilization efficiency was also indirectly confirmed by the presence of characteristic functional groups (–C–H and –C–O), nitrogen and carbon on the TiO2/ZnO/LTV biocatalytic surface, identified by spectroscopic analyses. The increase in the surface area to 126 m2/g, change of isoelectric point (2.0) and zeta potential ranges (from +12.0 to −20.0 mV) after the immobilization process were also observed. The results show that the designed biocatalytic system enables the removal of acid dyes (C.I. Reactive Black 5 and C.I. Acid Green 25) with high efficiency (99% and 70%, respectively). Mass spectroscopy analysis indicated possible degradation products formed by the cleavage of N=N and C–N bonds.