Formulation F2 Research Articles

Development and Characterization of Olmesartan Medoxomil-Loaded Microspheres for Hypertension Management

Our aim is to develop and assess microspheres loaded with olmesartan medoxomil, the antagonist of angiotensin II receptor which is used in hypertension treatment, for their efficacy. The microspheres were fabricated through a solvent evaporation process employing eudragit L100 and chitosan as the inner phase and liquid paraffin as the outer phase. Optimization was done according to the results of entrapment efficiency and in-vitro drug release. Fourier-transform infrared (FTIR) analysis indicated negligible interaction, which clarifies the suitability of the drug and excipients. The resulting microspheres exhibited a pale yellow hue and free-flowing characteristics, as confirmed by micromeritics experiments. Scanning electron microscopy (SEM) revealed smooth and spherical microspheres. Particle size, ranging from 187.44 to 358.75 μm, increased with polymer concentration, as determined by optical microscopy. Formulation F9, with a ratio of eudragit L100 to chitosan at 7:1, demonstrated the highest drug entrapment percentage (97.82%). In-vitro release studies demonstrated a reduction in olmesartan medoxomil release with increasing polymer content, with formulation F9 sustaining release for 12 hours. Furthermore, short-term accelerated stability testing indicated the physicochemical stability of the microsphere formulations throughout the stability period.

Formulation Optimization and Evaluation of Herbal Films Containing Ethanol Leaves Extract of Cassia auriculata to Treat Chronic Constipation Disorder

An intriguing trend in recent years has been the designing of oral films containing extracts from medicinal plants. Therefore, efforts were made in the current work to create fast-dissolving herbal films using Cassia auriculata ethanol leaf extract in order to create a dosage form that would be more convenient to administer and treat chronic constipation disorders in the elderly. Varying ratios of hydroxy propyl methyl cellulose as polymer, propylene glycol as film softener, and a solvent-casting approach were utilized to create the quickly dissolving herbal films of C. auriculata leaf extract. A number of quality control measures, including weight fluctuation, thickness variation, surface pH, percentage moisture uptake, percentage moisture loss, disintegration time and folding endurance, were assessed. According to the findings, every film had a decent appearance, a smooth texture, was free of particle matter, and had excellent folding endurance. According to a content uniformity analysis, the drug is dispersed evenly across the entire film, and each one dissolves in less than 95 seconds. In-vitro dissolving studies using Paddle type apparatus in pH 6.8 phosphate buffer pH 6.8, which is simulated saliva, were performed for each film composition. Out of all nine formulations, formulation F5, which is an herbal film with 10% propylene glycol and 40% HPMC, exhibited complete drug release (99.6%) in 30 minutes and had a strong folding endurance value. The release of medication from films was found to follow a first-order kinetics. Overall, studies indicate that the most feasible dose form that can be used in medical settings for the treatment of chronic constipation disorder is fast-dissolving herbal films containing C. auriculata leaves extract. This is especially true for patients who have difficulty swallowing.

Design and evaluation of oseltamivir phosphate dual-phase extended-release tablets for the treatment of influenza

In this study, once-daily extended-release tablets with dual-phase release of oseltamivir phosphate were developed for the treatment of influenza. The goal was to improve patient adherence and offer more therapeutic choices. The tablets were manufactured using wet granulation, bilayer tablet compression, and enteric membrane-controlled coating processes. Various polymers, such as hydroxypropyl methylcellulose (HPMC K100MCR, K15MCR, K4MCR, K100LV), enteric polymers (HPMC AS-LF, Eudragit L100-55) and membrane-controlled polymers (OPADRY® CA), were used either individually or in combination with other common excipients. The formulations include enteric-coated extended-release tablet (F1), hydrophilic matrix extended-release tablet (F2), semipermeable membrane-controlled release tablet (F3) and a combination extended-release tablet containing both enteric and hydrophilic matrix (F4). The in vitro drug release profile of each formulation was fitted to the first-order model, and the Ritger-Peppas model suggested that Fickian diffusion was the primary mechanism for drug release. Comparative bioequivalence studies with Tamiflu® (oseltamivir phosphate) capsules revealed that formulations F1, F2, and F3 did not achieve bioequivalence. However, under fed conditions, formulation F4 achieved bioequivalence with a relative bioavailability of 95.30% (90% CI, 88.83%-102.15%). This suggests that the formulation F4 tablet could potentially be a new treatment option for patients with influenza.

Formulation, design, and evaluation of valsartan sodium-sustained-release matrix tablets

The main aim of present work was to formulate and evaluate sustain release matrix tablets of Valsartan, an angiotensin II Receptor type 1 antagonist. Sustain release formulation are those which delivers the drug locally or systemically at a predetermined rate for a fixed period of time. The matrix tablet was prepared by direct compression method using by various concentration of chitosan and sodium alginate with combination of various release retardant polymer. The powder mixtures were subjected to various pre-compression parameters such as angle of repose, bulk density, tapped density and Carr’s index shows satisfactory result and the compressed tablets are evaluated for post-compression parameters such as weight variation, thickness, hardness, friability, drug content, in-vitro dissolution and stability studies. In-vitro dissolution studies were carried out for 24 hours using 0.1N HCl for first 2 hours and pH 6.8 phosphate buffers for 24 hours and the result showed that formulations F4 and F7 showed good dissolution profile to control the drug release respectively. Formulation containing higher concentration of chitosan and sodium alginate along with polymers sustainedthedrugreleasefor theperiodof24hours.The compatibilityof thedrug, polymers and other excipients were determined by FT-IR Spectroscopy. Results showed that the drug was compatible with polymers and other excipients. The release data was fitted to various mathematical models such as Zero-order, First-order, Higuchi equation and Korsmeyer- Peppas model to evaluate the kinetics and the drug release. The drug release followed first order and the mechanism was found to be non-Fickian. The stability studies were carried out for 3 months and result indicates that the selected formulations (F4and F7) were stable.

Preparation, Characterization and Evaluation of Antioxidant Flavonosomes

The objective of the present study was to prepare flavonosomes loaded with kaempferol and curcumin in order to improve the bioavailability of the flavonoids. The flavonosomes loaded with kaempferol and curcumin were prepared using bulk co-loading method using lecithin as the lipid molecule. The particle size of the flavonosomes was determined using zeta sizer and ranged from 497.3 nm to 167.1 nm. The results indicated that increase the ratio of lipid to extract was able to reduce the particle size of the flavonosomes. The flavonosomes prepared using 4:1 ratio of lipid to flavonoids were found to be rigid, spherical as seen in SEM with smooth regular surface. Sharp and distinct endothermic peaks in DSC revealed the formulation of stable flavonosomes due to molecular interactions between the extract and lecithin. The entrapment efficiency of flavonosome preparation F4 was determined by measurement of the non-entrapped flavonoids and subtracting from the total flavonoids used to obtain the flavonoids entrapped in the formulation. The entrapment efficiency of F4 has been calculated to be 94.12%. The flavonosome F4 was studied for release of the entrapped flavonoids by dialysis method. The amount of flavonoids released at 1, 2, 3, 4, 6, 8, 10 and 12 hours was determined using UV spectrophotometry. After the first hour, the entrapped flavonoids released in a steady manner from the flavonosome depicting and almost complete release (90.52% for kaempferol and 94.67% for curcumin) from the formulation. The flavonosomes were found to be stable under the storage conditions. The best formulation with respect to particle size and anti-inflammatory action was F4 that contained 4:1 ratio of lecithin: flavonoids. DPPH radical scavenging assay was used to determine the antioxidant action of the individual flavonoids and the flavonosome formulation. It was found that the formulation F4 was having higher antioxidant activity in comparison to kaempferol and curcumin. The IC50 of kaempferol, curcumin and flavonosome were found to be 228.20 µg/mL, 175.51 µg/mL and 158.19 µg/mL respectively. Keywords: Flavonosome, Kaempferol, Curcumin, Bulk co-loading, antioxidant

Production and evaluation of quality characteristics of ready-to-drink Aloe vera juice incorporation with ginger and lemon

The food and beverage industry are witnessing an increase in demand for health beverages. Globally, Aloe vera is well-known for its useful qualities and health advantages. The study was conducted to formulate a ready-to-drink Aloe vera juice from mature Aloe vera gel to examine biochemical properties, microbial analysis, and the sensory properties of the Aloe vera juice produced. Three formulations coded as F1, F2, and F3 were prepared. Fresh Aloe vera gel had the following properties: 98.49 % moisture, 0.15 % ash, pH 4.73 %, and 0.06 % acidity. Formulation F2 had the highest levels of total phenol, flavonoid, DPPH, and FRAP, while formulation F3 had greater levels of vitamin C and acidity. The finished products were preserved in clean, dry, and sterilized plastic bottles and stored in the refrigerator at 4 °C. The drink's TSS, acidity, pH, and vitamin C levels were all measured up to 60 days of storage. It was observed that during the storage periods, pH and vitamin C gradually decreased while TSS and acidity slightly increased. The minimal change in microbial activity was observed in formulation F3 while F2 obtained the highest scores in the sensory evaluation.

Synthesis, Characterization, and Stability Optimization of Ibuprofen Cocrystals eEploying Various Hydrophilic Polymers.

Cocrystals are an efficient way for the delivery of low soluble drugs but when dissolved they rapidly disproportionate. To formulate the cocrystals in tablets, cocrystals must be stabilized. In this study ibuprofen-nicotinamide (IBU-NIC) cocrystals were synthesized initially by slow solvent evaporation and for bulk production by fast solvent evaporation techniques. The cocrystals were characterized by powder X-ray diffraction (PXRD), Fourier transform infrared spectrophotometer (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and optical microscopy. The ibuprofen cocrystals showed greater solubility compared to the parent drug. Intrinsic dissolution data was utilized for efficacious screening of tablet formulations. Using hydrophilic polymers at a ratio of 6:1 (polymer to IBU-NIC cocrystal ratio), hydroxypropyl methylcellulose (F1), polyvinylpyrrolidone (PVP) K-30 (F2) and PVP K-90 (F3), three tablet formulations were prepared that stabilized cocrystals during dissolution. The drug release profiles after 60 minutes from formulations F1 (92.30), F2 (98.54), F3 (99.88) were all higher compared to the marketed brand BRUFEN® F, (79.61%) in a simulated intestinal media (p<0.001). Significant increase in the dissolution rate of cocrystal was observed with no phase change in all formulations.

Conversion of Sweet Whey to Bioethanol: A Bioremediation Alternative for Dairy Industry

In many countries, whey from the dairy industry is an abundant waste that generates an important environmental impact. Alternative processes to use the whey and minimize the environmental impact are needed. This work considered six formulations with different ammonium sulfate and L-phenylalanine (L-Phe) concentrations to produce bioethanol in sweet whey fermentation by Kluyveromyces marxianus. The results showed a maximum bioethanol concentration equal to 25.13 ± 0.37 g L−1 (p &lt; 0.05) for formulation F6, with 1 g L−1 of L-Phe and 1.350 g L−1 of ammonium sulfate (96 h). For these conditions, the chemical oxygen demand removal percentage (CODR%) was 67%. The maximum CODR% obtained was 97.5% for formulation F3 (1 g L−1 of L-Phe) at 96 h; however, a significant decrease in bioethanol concentration (14.33 ± 2.58 g L−1) was observed. On the other hand, for formulation, F3, at 48 h of fermentation time, a bioethanol concentration of 23.71 ± 1.26 g L−1 was observed, with 76.5% CODR%. Based on these results, we suggest that the best conditions to obtain a significant bioethanol concentration and CODR% value are those used on the configuration F3 at 48 h.

Formulation and evaluation of transdermal patch of carbamazepine

Transdermal drug delivery system (TDDS) is a widely accepted mode of drug delivery method due to various advantages and one of the novel routes for systemic delivery of drugs through intact skin. Topical drug administration is a systemic and localized method of delivering drugs through skin and is considered an attractive alternative to oral and parenteral routes. The aim of present study was to formulate and evaluate Matrix type transdermal drug delivery system (TDDS) of Carbamazepine was prepared by the solvent evaporation technique. Several batches were prepared by using combination of HPMC E-15, Eudragit RL-100, and Ethyl Cellulose different ratios. Propylene glycol was used as plasticizer and DMSO was incorporated as a permeation enhancer. These Formulated transdermal patches were characterized for their physicochemical parameters like thickness, weight variation, folding endurance, percentage moisture uptake, Percentage moisture uptake and In vitro drug release studies were examined. Among the above all formulation F6 was chosen as a best Formulation, because this optimised formulation showed satisfactory drug content, physical characteristic for its thickness, weight uniformity, percentage moisture content, percentage moisture uptake, and maximum % of drug release i.e., 93.95 % in 12 hours. The optimized formulation (F6) showed maximum highest percentage of drug release.

FORMULATION, CHARACTERIZATION AND IN-VITRO EVALUATION OF FLOATING MICROSPHERE OF IBUPROFEN USING CARBOPOL 940 POLYMER

In this study, ibuprofen hollow microspheres are prepared and assessed using a novel emulsion-solvent diffusion process in an effort to increase the drug's enteric bioavailability by extending the duration of the drug's stomach residence. Carbopol 940, drug, ethanol, and the DCM solution were added to an agitated PVA aqueous solution that was thermally regulated to 40 degrees Celsius to create microspheres. The resultant microspheres were separated through filtration and subjected to various evaluations like micrometrics characteristics, morphology, in vitro floating behaviour, percentage of drug entrapment, and in vitro drug release. According to in vitro release experiments, formulation F3 was found to be 86.75 % in 10 hrs. It is possible to draw the conclusion from the study that microspheres are the perfect tool for increasing the length of time a drug is present in the stomach and improving its enteric bioavailability.

Ethnobotanical Study and Hedonic Evaluation with Cost Analysis of Banana (Musa paradisiaca L.) Stem Serum Preparation as an Anti-Aging Solution

In skincare, particularly facial serums, the utilization of natural ingredients is crucial in addressing various skin issues, notably combating the effects of free radicals that contribute to wrinkles. This study explores the potential of banana (Musa paradisiaca L.) stem extract as an active ingredient in serum formulation due to its rich anthocyanin content known for antioxidant properties. Hedonic testing and cost analysis serve as initial steps in the marketing mix of a product. This research aims to assess the hedonic preferences of various M. paradisiaca stem serum formulations and analyze the production costs. A descriptive research method employing survey and observational techniques was utilized for data collection and descriptive analysis. Hedonic testing was conducted to gauge the personal preferences of panelists toward M. paradisiaca stem serum formulations. Three formulations (F1 with 4%, F2 with 8%, and F3 with 12% M. paradisiaca extract) were evaluated by 40 panelists. Cost analysis of serum production employed quantitative descriptive analysis, computing the cost per unit using a variable costing method. The hedonic evaluation results showed that F1 formulation was highly preferred (79.3%), followed by F2 (73.2%), and F3 (66.8%). Cost analysis using the variable costing method revealed a total production cost of IDR 614,000.00 for 10 packages of M. paradisiaca stem serum formulation, translating to an approximate unit price of IDR 61,400.00.

Formulation and evaluation of emulgels loaded with microspheres containing Baricitinib

The main objective of the present research work was to formulate and evaluate transdermal gel loaded with microspheres of Baricitinib to increase bioavailability and to reduce the dosing frequency and to improve patient compliance. Gel loaded with microspheres of Baricitinib was prepared by taking different ratios and grades of Carbopol polymers. The prepared formulations (F1–F9) were evaluated for pre-formulation studies, percentage yield, particle size, content Uniformity, drug content entrapment efficiency and in vitro dissolution studies. The optimized gel loaded with microspheres of F8 formulation (drug: Carbopol 974polymer in 1:1 ratio) is more effective compared to all formulations. The prepared gel showed acceptable physical properties such as particle size of (126.5 microns), percentage yield of (96.5%), content uniformity (97.8), and drug content entrapment efficiency (90.5%). In vitro dissolution studies have shown 100.1% drug release in 12 h. With the optimized formulation Baricitinib emulgels are formulated using different grades and ratios of Carbopol and optimized microsphere formulation F8. The Emulgel formulation F7 showed the acceptable results with a yield of 92.3%, Drug content (100.2%), Spread ability (13.38 g.cm/s), Viscocity (112.3 cP), pH off 6.05 and it was observed that formulation F7 showed 100.2% drug release within 12 hours. All the results show that the gel loaded with microspheres of Baricitinib can be effectively used for the treatment of viral infections like small fox.

Preparation and Evaluation of Metronidazole Tablets Produced with Different Binders Using Wet Granulation Method

In tablet formulation, binders are essential for ensuring proper powder mix, granulation and overall tablet quality. Variations in binder quality and concentration can impact drug bioavailability, strength and manufacturing processes. The inconsistency in bioavailability and therapeutic response of metronidazole from different manufacturers highlights the importance of binder selection in tablet formulation. This study evaluates the impact of different binding agents on tablet quality. The optimum binder concentration for each of the binders was assessed to obtain suitable concentration that was used to prepare metronidazole tablets. Metronidazole tablets were formulated with four different binder vis, acacia, gelatine, PVP, maize starch at 3% concentration using wet granulation method after which the tablet properties were evaluated. Metronidazole powder exhibited poor flow indices, as indicated by angle of repose: 39.92 ± 1.85, Carr’s compressibility index (CI): 20.13 ± 0.28 and Hausner’s ratio (Hr): 1.26 ± 0.01, whereas its granules exhibited good flow properties. The crushing strength (CS), friability (FR), disintegration time (DT) (CSFR/DT) ratio for batches showed values in 3% binder concentration, indicating higher strength as compared to other concentrations. There was a significant increase (P &lt; 0.05) in the CSFR/DT ratio for gelatine (2.22) in formulation F2 compared to maize starch in Formulation F4. The formulated tablets with the various binders have met with the British Pharmacopeial criteria of 80% drug release from uncoated immediate-release tablets. Amongst the four binders, gelatine was found to be the best in the formulation of robust metronidazole tablets by wet granulation method at an optimised concentration of 3% w/w. Tablets produced with gelatin exhibited greater mechanical strength than those produced with other binders, while also demonstrating a slightly longer DT. Metronidazole tablets produced with gelatine have met the British Pharmacopeial requirements including an acceptable in-vitro drug release profile.

Effect of Edge Activator Combinations in Transethosomal Formulations for Skin Delivery of Thymoquinone via Langmuir Technique

Thymoquinone (TQ), a bioactive compound found in Nigella sativa seeds, possesses diverse therapeutic properties for skin conditions. However, formulating TQ presents challenges due to its hydrophobic nature and chemical instability, which hinder its skin penetration. Transethosomes, as a formulation, offer an environment conducive to enhancing TQ’s solubility, stability, and skin permeation. To optimize TQ transethosomal formulations, we introduced a combination of ionic and nonionic surfactants, namely Tween 20 and sodium lauryl sulfate (SLS) or sodium lauroyl glutamate (SLG). Surfactants play a crucial role in stabilizing the formulation, reducing aggregation, improving biocompatibility, and minimizing potential toxicity. We fine-tuned the formulation composition and gained insights into its interfacial behavior using the Langmuir monolayer technique. This method elucidated the interfacial properties and behavior of phospholipids in ethosome and transethosome formulations. Our findings suggest that monolayer studies can serve as the initial step in selecting surfactants for nanocarrier formulations based on their interfacial dilational rheology studies. It was found that the addition of surfactant to the formulation increased the elasticity considering the capability of transethosomes to significantly decrease their radius when permeating the skin barrier. The results of the dilational rheology experiments were most relevant to drug permeation through the skin for the largest amplitude of deformation. The combination of Tween 20 and SLS efficiently modified the rheological behavior of lipids, increasing their elasticity. This conclusion was supported by in vitro studies, where formulation F2 composed of Tween 20 and SLS demonstrated the highest permeation after 24 h (300.23 µg/cm2). Furthermore, the F2 formulation showed the highest encapsulation efficiency (EE) of 94%, surpassing those of the control and ethosomal formulations. Additionally, this transethosomal formulation exhibited antimicrobial activity against S. aureus, with a zone of inhibition of 26.4 ± 0.3 mm. Importantly, we assessed the cytotoxicity of both ethosomes and transethosomes at concentrations ranging from 3.5 µM to 50 µM on HaCaT cell lines and found no cytotoxic effects compared to TQ hydroethanolic solution. These results suggest the potential safety and efficacy of TQ transethosomal formulations.

Development of novel 3D printable inks for protein delivery

The application of 3D printing technology in the delivery of macromolecules, such as proteins and enzymes, is limited by the lack of suitable inks. In this study, we report the development of novel inks for 3D printing of constructs containing proteins while maintaining the activity of the proteins during and after printing. Different ink formulations containing Pluronic F-127 (20–35 %, w/v), trehalose (2–10 %, w/v) or mannitol, poly (ethylene glycol) diacrylate (PEGDA) (0 or 10 %, w/w), and diphenyl(2,4,6-trimethylbenzoyl) phosphine oxide (TPO, 0 or 0.2 mg/mL) were prepared for 3D-microextrusion printing. The F2 formulation that contained β-galactosidase (β-gal) as a model enzyme, Pluronic F-127 (30 %), and trehalose (10 %) demonstrated the desired viscosity, printability, and dose flexibility. The shear-thinning property of the F2 formulation enabled the printing of β-gal containing constructs with a good peak force during extrusion. After 3D printing, the enzymatic activity of the β-gal in the constructs was maintained for an extended period, depending on the construct design and storage conditions. For instance, there was a 50 % reduction in β-gal activity in the two-layer constructs, but only a 20 % reduction in the four-layer construct (i.e., 54.5 ± 1.2 % and 82.7 ± 9.9 %, respectively), after 4 days of storage. The β-gal activity in constructs printed from the F2 formulation was maintained for up to 20 days when stored in sealed bags at room temperatures (21 ± 2 °C), but not when stored unsealed in the same conditions (e.g., ∼60 % activity loss within 7 days). The β-gal from constructs printed from F2 started to release within 5 min and reached 100 % after 20 min. With the design flexibility offered by the 3D printing, the β-gal release from the constructs was delayed to 3 h by printing a backing layer of β-gal-free F5 ink on the constructs printed from the F2 ink. Finally, ovalbumin as an alternative protein was also incorporated in similar ink compositions. Ovalbumin exhibited a release profile like that of the β-gal, and the release can also be modified with different shape design and/or ink composition. In conclusion, ink formulations that possess desirable properties for 3D printing of protein-containing constructs while maintaining the protein activity during and after printing were developed.

Formulation and evaluation of immediate-release capsules of pregabalin

The aim is to develop and evaluate capsules with various excipient compositions that satisfy the reference product's specifications to achieve an in-vitro correlation with the reference product after that. Pregabalin I.R. capsules were formulated using Corn starch, Dibasic calcium phosphate, Lactose anhydrous, and Avicel pH 102(Microcrystalline cellulose). After compatibility studies for the capsule blend were completed, the Drug was determined to be compatible with all excipients used in various formulations. After the blend was put into capsules, several metrics were examined, including average weight, disintegration, and assay. The formulation containing D.C.P. disintegrates at a faster rate than other formulations. It was discovered that the percentage of drug release in the F7 invitro dissolving profile was equal to that of the innovator product. Finally, it was concluded that the F7 formulation is better and similar to the innovator product.

Formulation and Evaluation of Betulin Loaded Transdermal Patches

Objectives: To develop and evaluate Transdermal patches of Betulin along with various polymers for controlled release action. Method: Suitable method such as Solvent Casting Technique of Film Casting Technique are used for preparation of Transdermal patch. Result: The prepared Transdermal patches were transparent, smooth, uniform and flexible. The method adopted for preparation of system was found satisfactory. Conclusion: Various formulations were developed by using hydrophilic and hydrophobic polymers like HPMC E5 and EC respectively in single and combinations by solvent evaporation technique with incorporation of penetration enhancer such as dimethylsulfoxide and dibutyl phthalate as plasticizer. Formulation F7 containing equal ratio of HPMC E5: EC (5:5) showed maximum percentage drug content 95.44%. A suitable UV Spectroscopy method for the analysis of Betulin was developed. Betulin showed maximum absorption at wave length 215 nm in isotonic phosphate buffer (pH 7.4) solutions. The pre-formulation studies involving description, solubility, melting point, partition coefficient of the drug were found to be comparable with the standard. The Transdermal patch of Betulin was prepared successfully by solvent evaporation method. Transdermal patch of Betulin for Transdermal drug delivery was evaluated. Calibration curve was obtained; Transdermal film was prepared, overcome limitations regarding bioavailability of drug was done. Keywords: Controlled DDS, Transdermal DDS, Betulin, Transdermal Patch, solvent evaporation method.

Formulation, Evaluation, and Characterization of Indapamide Niosomes

Niosomes, also known as nonionic surfactant vesicles, are one of the many carriers used to carry drug molecules to their target sites. They can hold both hydrophilic and hydrophobic medicines. Indapamide is an angiotensin II type 1 receptor (AT1) antagonist medication primarily used to treat high blood pressure. Niosomes containing Indapamide were created utilizing the thin film hydration process with various cholesterol concentrations and nonionic surfactants (span 60). All noisome formulations were assessed for entrapment efficiency, drug content, reproducibility, vesicular diameter, shape and size distribution microphotography, FTIR analysis, and in vitro release experiments. The results indicate that in all of the created niosomal formulations, as the surfactant content increases, the entrapment efficiency also increases. The drug content ranged between 90.06±0.57 and 96.15±0.42, with a low standard deviation. Niosomes range in size from 0.280±0.098µm to 0.299±0.044µm and have a spherical shape. The IR spectrum analysis indicated no interaction between the medication and the formulation ingredients. Membrane diffusion cells were used to study the in vitro dissolution parameters. The results demonstrate that formulation F6 had a better-controlled release action than other formulations, with an 'n' value of 0.917, indicating that the medication was released using zero-order kinetics.

FORMULATION DEVELOPMENT AND IN VITRO PENETRATION TEST OF ETHOSOME OF CHROMOLAENA ODORATA LEAVES EXTRACT

Objective: This study aimed to develop and assess ethosome preparation using extracts derived from the leaves of Chromolaena odorata. Methods: The study started by obtaining Chromolaena odorata leaf extracts. Furthermore, Ethosome formulations were produced using a thermal technique. Ethosome variants were created, each with distinct compositions: Formulation F1, containing 10 ml of ethanol without the extract; Formulation F2, consisting of 0.5 grams of the extract mixed with 10 ml of ethanol; Formulation F3, combining 1 gram of the extract with 20 ml of ethanol; and Formulation F4, incorporating 1.5 grams of the extract with 30 ml of ethanol. The ethosomal systems were thoroughly characterized using various analytical techniques, such as organoleptic analysis, quantification of particle dimensions, zeta potential evaluation, pH metric analysis, transmission electron microscopy (TEM) imaging, and in vitro permeability assessment using the Franz Diffusion Cell apparatus. Results: The findings indicated that the optimized F4 formulation showed 161.2±32.0 nm particle size measurement and a+34.33±0.58 mV zeta potential. All formula possess a pH range of 4.5-6.5, within which the skin can acclimate to preparations. It is evident from all formulations that the pH decreased after the addition of the extract at an acidic pH of 4.11. Following the 12-week storage period, the pH of all treatments exhibited a modest reduction; however, it remained within the acceptable range for skin pH. Furthermore, the F4 formula also had a higher level of penetration activity. Conclusion: The optimized ethosomal formulations of Chromolaena odorata have promising applications in enhancing the permeability and efficacy of plant-derived therapeutic agents.

The Formulation, Development And Evaluation Of Ointment For Anti-Inflammatory Activity

The search for safer anti-inflammatory agents has led to exploration of natural sources such as curcumin and fenugreek. Curcumin, derived from Curcuma longa, and α-linolenic acid from Trigonella foenum-graecum, exhibit significant anti-inflammatory properties. This study focuses on formulating an ointment utilizing these extracts for topical application. Molecular docking techniques were employed to assess the binding affinities of curcumin and α-linolenic acid. The ointment was prepared using various bases and preservatives, and its physicochemical properties were evaluated. Stability studies revealed consistent properties under different temperature conditions. Characterization of the drug extracts and ointment formulations was conducted to ensure efficacy and safety. The ointment showed promising results in terms of stability and efficacy, particularly formulation F2, suggesting its potential as a topical anti-inflammatory therapy with improved patient compliance