Formulation F2 Research Articles

Formulation and Evaluation of Mucoadhesive Buccal Tablets of Carvedilol

The aim of the study was to formulate and evaluate the carvedilol buccal tablets using HPMC K4M and xanthan gum as polymer. Buccal tablets of carvedilol were prepared by direct compression technique by using polymer in combination at different concentration. Drug excipient compatibility study indicates that there is no interaction between the excipient and the drug. Total seven batches were prepared and subjected to evaluation parameters. Pre-compression parameters for all batches showed excellent flow propertied of powder bled. Prepared buccal tablets were evaluated for various post compression parameters like hardness, thickness, weight variation, drug content, and friability, % swelling index, muco-adhesive strength and in vitro drug release. The harness of all batches was optimum showed good mechanical strength; thickness of tablets was uniform in all formulations the weight variation test of all the formulation was found to be within the limits of pharmacopoeial standard. % swelling index for all the batch formulation was optimum and seen to increase with increase in polymer concentration. Mucoadhesive strength was also showed acceptable results for all batch formulations which satisfy the need of mucoadhesive tablets. The in vitro dissolution profile of all the formulation showed sustained release of drug, for extended periods of time. The optimized formulation of F4 prepared with was consider as the optimized formulation with respect to drug content, % swelling index, Mucoadhesive strength and in vitro drug release pattern for 8 hrs. Formulation F4 showed highest 98.32±1.55 % drug release at the end of 8 hrs. Optimized formulation F4 was found to be stable during the stability studies for 3 month indicating good stability of the formulation. Keywords: carvedilol, Mucoadhesive strength, Optimized formulation, buccal tablets.

Formulation and Evaluation of Herbal Hand Sanitizers Based on Plants Producing Essential Oil

Hand hygiene is important because it can easily be transmitted through direct contact with microbial spores produced during coughing and sneezing. It is important to prevent the spread of the disease, especially in cases such as epidemics, through the use of antibiotics. This can be achieved by establishing and maintaining strict infection control equipment such as good hygiene in hospitals and public places. The aim of this study is to prepare an alcohol-based sanitizer against bacterial infections. After the test, the pH value of the disinfectant is between 6.65 and 6.67. The viscosity of the antiseptic is between 389 cps to 835. The spread ability was good and found in range between 6.55 to 7.18 g-cm/sec. The drug content of Eucalyptus Oil in formulations was found to be 93% in F1 and 97.5% in F2. In-vitro drug release study was found to be 56.2% in F1 and 60.6% in F2, and the stability of the preparation remained stable after 3 months of storage. All these studies showed that the F2 formulation is the best as it has better pH, viscosity, spreading ability and safety.

EFIKASI DAN EFEKTIVITAS FORMULASI DAUN MELADA (Piper colubrinum Link) SEBAGAI ATRAKTAN HAMA LALAT BUAH (STUDI KASUS PERTANAMAN CABAI)

Fruit flies ( Bactrocera spp.) represent a group of Plant Pests that can inflict both qualitative and quantitative losses. The utilization of chemical pesticides and the scarcity of Methyl Eugenol continue to pose significant challenges in agriculture. The abundant availability of Melada plants presents an opportunity for the development of an economically viable and environmentally friendly biological attractant. Encapsulation technology based on Maltodextrin and Gum Arabic (MD-GA) formulated with powdered simplicia of Melada leaves F1(02:10), F2(05:10), F3(10:10), and F4(12:10) is employed to enhance the slow-release resistance of volatile compounds. The surface oil content of the four formulations ranges from 0.3% to 9.6%. The encapsulation efficiency value for the four formulations ranges from 70% to 85%. The loading capacity value ranges from 0.7% to 1.3%. The yield value of microcapsule characteristics ranges from 63% to 82%. Morphological analysis reveals a decrease in the number of particles along with the combination of treatment formulations. The size of the microcapsules for the four formulations falls within the range of 201.2 µm–252.6 µm. The effectiveness of the resulting attractant can lure 19-185 fruit flies. The diversity of the fruit fly pest population obtained includes the Bactrocera umbrosa and Bactrocera melastomatos species. The total value of the best formulation for the four treatments ranged from 0.3% to 0.5%. The optimization of the best biological attractant application with high development potential lies in the encapsulation formulations F3 and F4.

Formulation and evaluation of herbal essential oil based nail lacquer for management of onychomycosis

IntroductionOnychomycosis (Paronychia) is a common fungal nail infection, characterised by thickened, discoloured and brittle nails often accompanied by pain and discomfort. It is one of the most prevalent fungal nail infections with the global incidence of >20 % affected commonly by Candida albicans and Candida parapsilosis. The market today is flooded with various antifungal therapies (Azoles, Imidazoles, Allylamines, etc.) but their clinical applicability is limited due to associated side effects. The study is an attempt to formulate essential oil-based nail lacquer against Candidal Onychomycosis. Material and MethodSelection of essential oils and preparation of their blends (EOB) was made on basis of their antifungal activity (minimum inhibitory concentration; MIC and zone of inhibition; ZOI) and physiological effect they exhibit on varied pathological parameters of onychomycosis. Simultaneously, varied batches of nail lacquer (N1-N5) were prepared by varying the concentrations of polymer and film forming agent and were evaluated for their formulatory characteristics (drying time, incidence of white patches, film texture, etc.). Optimal nail lacquer batch was loaded with screened EOB and was evaluated for various characteristics and antifungal activity. ResultThe formulation F4 was found to form a smooth, transparent film over the nail with absence of any tackiness or white patches. Moreover, F4 formulation exhibited minimum MIC among varied batches and higher ZOI (4.3 cm) as compared to marketed preparation (3.5 cm), indicating better antifungal activity. ConclusionEssential oils, as an active agent, could prove to be a natural, safer, and more effective alternative to the conventionally available topical preparations for the management of fungal infections. The development of this herbal mixture opens up new possibilities for treating onychomycosis, necessitating additional research and clinical studies to establish its clinical safety, efficacy, and viability.

Fabrication and Characterisation of Oral Fast-Dissolving Film of Metoprolol Succinate

Introduction: Oral, fast-dissolving films are an excellent alternative. The purpose of adopting the solvent casting approach was to create a compelling oral film. Methodology: HPMC E15 and sodium alginate polymers were chosen based on their compatibility. The produced films were evaluated in terms of organoleptic characteristics, weight, thickness, folding durability, tensile strength, drug content homogeneity, surface pH, disintegration time, and in-vitro dissolution kinetics. Results: Among the formulations, F2 had a disintegration time of 14.2 seconds and a phenomenal drug release of 98% in 5 minutes. As a result, formulation F2 emerged as the best option, demonstrating promising qualities for effective drug delivery. Conclusion: These films are made of thin strips and are easily applied to the tongue or oral mucosal tissue. When they come into contact with saliva, they quickly hydrate and attach, resulting in rapid medicine administration. Fast-dissolving oral films are an excellent alternative for patients who have difficulty swallowing traditional drugs, such as pediatric, geriatric, bedridden, or developmentally impaired people. These films are made of thin strips and are easily applied to the tongue or oral mucosal tissue. When they come into contact with saliva, they quickly hydrate and attach, resulting in rapid medicine administration. other: Nil

Sublingual Fast-Dissolving Thin Films of Loratadine: Characterization, In Vitro and Ex Vivo Evaluation.

Loratadine (LOR) is a second-generation antihistamine that exhibits a low and variable oral bioavailability (10-40%) and delayed onset owing to poor solubility and an extensive first-pass effect. Therefore, in light of the clinical need, the main goal of the present study was to develop sublingual fast-dissolving thin films of LOR-citric acid co-amorphous systems (LOR-CAs) with the aim of eliciting a faster onset and improving the bioavailability. We formulated sublingual fast-dissolving thin films of LOR by a film-casting technique using hydrophilic polymers like hydroxypropyl methylcellulose (HPMC E15), polyvinyl pyrrolidone K30 (PVP K30), and hydroxypropyl cellulose EL (HPC-EF) and citric acid as a pH modulator, while glycerin served as a plasticizer. The sublingual fast-dissolving thin films were characterized by FTIR, SEM, DSC, and XRD and evaluated for in vitro dissolution and ex vivo mucoadhesion. The best formulation (F1) developed using HPMC E15 as a polymer, glycerin as a plasticizer, and citric acid as a pH modulator was found to be the optimized formulation as it was smooth, clear, flexible, and displayed good mucoadhesion (11.27 ± 0.418 gm/cm2) and uniform thickness (0.25 ± 0.02 mm). The formulation F1 was found to display a significantly shorter DT (30.30 ± 0.6 s) and rapid release of LOR (92.10 ± 2.3% in 60 min) compared to other formulations (ANOVA, p < 0.001). The results indicated that the prepared sublingual films are likely to elicit a faster therapeutic effect, avoid first-pass metabolism, and improve the bioavailability.

Nutritional and functional synergism of Spirulina and açai mixtures in gummy candies

The compounds and properties of açai pulp and Spirulina biomass may suggest complementary and synergistic potential when combined. The aim of this work was to develop sucrose-free and dye-free gummy candies enriched with mixtures of freeze-dried açai pulp (FDAP) and Spirulina biomass. Four formulations were prepared: F1, 3% FDAP and 1% Spirulina; F2, 1% FDAP and 3% Spirulina; F3, 2% FDAP and 2% Spirulina and C, 0% FDAP and 0% Spirulina. The nutritional and functional contents, texture properties, color parameters and sensory characteristics of the gummy candies were assessed. Compared with the control, formulation F2 had the greatest increase in protein content (16.3%), whereas formulation F1 presented the greatest increase in lipid content (2.0%) and the greatest increase in total phenolic content (0.254 mg GAE g−1). Although the texture properties and the color parameters were significantly influenced (p < 0.05), the sensory evaluation showed a satisfactory acceptability index (AI) for the three formulations F1 (77.8%), F2 (82.8%), and F3 (80.1%). Thus, it was concluded that mixtures of Spirulina biomass and FDAP have a synergistic effect and could be combined as an innovative gummy candy formulation based on natural ingredients with incorporated bioactive compounds.Graphical

Simvastatin and adenosine-co-loaded nanostructured lipid carriers for wound healing: Development, characterization and cell-based investigation

Chronic wounds represent a significant global health burden, characterized by delayed skin healing and associated comorbidities. The present study aimed to develop nanostructured lipid carriers (NLCs) as a topical delivery system for the co-administration of simvastatin and adenosine to address chronic wound management. The rationale behind the co-delivery approach was to mitigate the cytotoxicity associated with high-dose simvastatin, while preserving its therapeutic benefits through a potential synergistic or additive effect. A significant challenge in the development of these NLCs was the encapsulation of the highly hydrophilic adenosine within the hydrophobic lipid matrix. The NLCs were prepared using a hot homogenization-sonication method with a double emulsion technique and optimized through a series of formulation trials, employing various surfactants, solid and liquid lipids, to achieve efficient drug encapsulation, particularly for the hydrophilic adenosine. Optimized formulations F5- and F10-S/A 0.6 %/2 % (containing 0.6 % simvastatin and 2 % adenosine), exhibited promising physicochemical properties. The main difference was the liquid lipid used: F5 containing Miglyol 810 N, while F10 Capmul MCM C-8. Both formulations displayed a mean particle size below 230 nm, a polydispersity index (PDI) of approximately 0.2, and a zeta potential of around –22 mV. While simvastatin association efficiency (AE) was nearly 100 %, adenosine AE was higher for F10 (24 %), compared to F5 (13.5 %). F5 demonstrated superior stability compared to F10, maintaining consistent particle size and PDI over a 60-day period. Formulation F5 also demonstrated superior cell-based in vitro performance compared to F10, with higher cell viability (MTT assay), greater cell proliferation induction (SRB assay), and enhanced cell proliferation and migration in the wound-scratch assay. While F10 displayed higher adenosine AE, F5 excelled in terms of stability and biological activity. The slightly increase in intracellular reactive oxygen species levels observed with F5 may contribute to its enhanced proliferative effects. In-depth characterization revealed that F5 comprised spherical nanoparticles, and thermal analysis indicated no significant changes in the nanocarrier structure upon drug encapsulation. Additionally, ex vivo permeability study demonstrated superior skin retention of both simvastatin and adenosine for F5 compared to an emulsion control. Overall, the F5 nanocarrier demonstrated suitable physicochemical properties, cellular biocompatibility, induction of cell proliferation and migration events, and drug retention capacity in the skin layers, indicating its potential as a promising topical treatment for difficult-to-heal wounds.

Formulation and evaluation of physical stability and antidiabetic activity from nanoliposomes containing an ethyl acetate extract of Solanum xanthocarpum Schrader &amp; Wendland fruit in rats

Introduction: The extract of Solanum xanthocarpum fruit has antidiabetic activity. This research aims to formulate nanoliposomes containing ethyl acetate extracts of S. xanthocarpum selected from multilevel extraction, evaluate their physical stability and antidiabetic activity, and compare them with the extract. Methods: The extracts were prepared using n-hexane, ethyl acetate, ethanol, and water as solvents, and their antidiabetic activities were evaluated to select the extract most effective in lowering blood sugar levels in rats. That extract was formulated into three nanoliposomes using varying amounts of phospholipid, cholesterol, and Span 60, i.e., F1 (40 mmol), F2 (50 mmol), and F3 (60 mmol). Various sonication times ranging from 10 to 30 minutes were evaluated for particle size, entrapment efficiency, and physical stability. The selected formulations were evaluated for antidiabetic activity. Results: The ethyl acetate extract showed the highest decrease in glucose in rats and was selected for nanoliposome formulation. The nanoliposomes obtained were physically stable at low temperatures for 12 weeks. F2 had the smallest particle size (143.97 nm) and the greatest entrapment efficiency (92.981% ± 0.35%) with a sonication time of 30 minutes and was significantly different from F1 and F3 (P&lt;0.05). The highest percentage reduction in blood sugar levels was with F2 at 74.57% and significantly differed (P&lt;0.05) from the ethyl acetate extract of S. xanthocarpum at 73.98% and the positive control rat group. Conclusion: The results show the potential uses of the prepared nanoparticles, especially the F2 formulation, as an antidiabetic formula.

Preclinical approaches to evaluate Uncaria tomentosa bark extract loaded FDOFs using osteoarthritis models

Osteoarthritis (OA) is one of the biggest global health issues, affecting two thirds of the population and cannot be fully treated to return normal function or relieve joint discomfort. Oral fast-dissolving films offer a high medication loading capacity, targeted distribution, and increasing bioavailability. The current research explores the in vitro and in vivo efficacy of oral fast-dissolving film formulations containing Uncaria tomentosa bark extract. A three-dimensional osteoarthritis (OA) model was created for in vitro assessment using first passage chrondrocytes cultured in a 1:1:3 ratio on trypsin-EDTA medium. C20A4 chondrocytes were cultured on agarose gel at 25± 5 °C in a phosphate buffer solution to create the OA agarose model. One milliliter of RPMI-1640 (10 % FBS) was used for chrondrocyte cultivation. On the third day of incubation, a 20 % (IL-1β) solution was applied, and the media was periodically changed. On the fifth day of incubation, the treated cell line received 5 μL of 0.5 % MTT reagent, and absorbance was examined at 570 nm. The effects of FDOFs on the cell lines were examined for 7, 13, 27, and 35 days (IL-1β, F5, F13 treated IL-1β injected types and Control). As a control, chondrocytes in agarose constructs were solely grown in RPMI-FBS medium without IL-1β. The arthritic effect of improved FDOFs, i.e., F5, was investigated using the GAG, HYP, and DNA quantitation assays in conjunction with a DNA content assay. Monoiodoacetate (MIA) produced arthritis models are well-established for understanding weight bearing and reaction to tactile stimuli in invivo research. Seven-week-old male wistar rats were used in the invivo technique, with celecoxib serving as the positive control and MIA as the negative control. Estimates of osteoarthritic potential were made based on the evaluation of knee thickness and discomfort. The study's findings demonstrated the effectiveness of the F5 formulation on OA models, which need for a clinical evaluation in human beings.

Evaluation of Physical Attributes and Efficacy of Lip Balm Formulated with Okra Fruit Extract (Abelmoschus esculentus (L.) Moench)

The okra fruit (Abelmoschus esculentus (L.) Moench) is renowned for its significant antioxidant properties, attributed to its rich content of bioactive compounds. Despite its high antioxidant activity, which has been extensively documented, its potential as a component in cosmetic formulations particularly lip balm preparation remains underutilized. This study seeks to address this gap by incorporating okra fruit extract into lip balm formulations and evaluating the resultant physical and functional attributes. Lip balm formulations were developed with three varying concentrations of okra fruit extract: F1 (1%), F2 (3%), and F3 (5%). A series of comprehensive evaluations were conducted to assess the physical stability and performance of the lip balms, including organoleptic properties, homogeneity, pH, melting point, spreadability, and overall stability. Stability was monitored over a 28-day period at room temperature to simulate typical storage conditions. The antioxidant efficacy of the okra extract was quantified using the DPPH (1,1-diphenyl-2-picrylhydrazyl) assay, which yielded an IC50 value of 10.06 ppm, reflecting its potent free radical scavenging capacity. The lip balm formulations exhibited a distinct okra aroma, smooth texture, and uniform color variations ranging from light brown (F1), brown (F2), to dark brown (F3). pH values ranged from 5.40 to 5.81, and melting points were between 49.6°C and 52.9°C, all within the acceptable range as per SNI 16-4769-1998 standards. ANOVA statistical analysis revealed no significant changes (p &gt; 0.05) in melting point and spreadability over time. However, significant differences (p &lt; 0.05) were noted in pH values, with further analysis indicating that formulations F2 and F3 differed significantly from F1 (p &lt; 0.05). These results demonstrate that okra fruit extract not only enhances the antioxidant properties of lip balm but also maintains its stability and functionality, supporting its potential as a valuable ingredient in cosmetic formulations.

Formulation and Evaluation of Lungs-Specific Doxorubicin-Loaded Chitosan-PLGA-Alginate Polymeric Nanoparticles

Background: An antibiotic called doxorubicin is produced by the Streptomyces peuce-tius bacterium, which is a member of the anthracycline drug class and is used in chemotherapy. Usually, doxorubicin is employed to cure solid tumors in children and adult patients. The physical and biological stability of the medicine can be increased by encasing it in nanoparticles, which increases the active pharmaceutical ingredient's bioavailability. Objective: This study aimed to create lungs targeting doxorubicin-loaded biodegradable polymer-ic nanoparticulate system by utilizing an appropriate method and conducting its evaluation. Methods: The polymeric nanoparticles using biodegradable polymers were prepared by the emul-sion polymerization method. Franz- diffusion cells were utilized to conduct in-vitro drug diffu-sion investigations. Results: Based on the outcomes of the experiments carried out for the research, polymeric nano-particles of doxorubicin were prepared utilizing different concentrations of chitosan, Sodium al-ginate, and PLGA. The visual appearance of doxorubicin polymeric nanoparticles shows homo-geneous dispersion with no phase separation form. The percentage yield, % entrapment efficien-cy, and drug content obtained for the final formulation were 93.43 ± 1.776, 87.31 ± 1.075, and 91.98 ± 0.493, respectively. A size dimension of 174.51 nm with a PDI of 0.242 and zeta poten-tial value of -36.1 mV of prepared nanoparticles demonstrate the stability of the formulation. The presentation of the PNPs of the optimized formulation having 310mg Tween 80 showed in vitro diffusion of 98.93% ± 0.296 % and an increased flux rate. Based on the determination coeffi-cients, the Higuchi model (K0 = 20.43 and R2= 0.982) was determined to have the best fit for the release data. Conclusion: Based on the trials conducted during the investigation, it was determined that the emulsion polymerization technique was best for the fabrication of the polymeric nanoparticles by utilizing different concentrations of chitosan, Sodium alginate, and PLGA. The formulation F6 containing 310mg Tween 80 suggested improved in vitro diffusion following the Higuchi model throughout all formulations. The findings suggest that a sustained process was responsible for the drug's release from the doxorubicin polymeric nanoparticles.

Design, Formulation, and Optimization of Nicardipine-Loaded Gastroretentive Floating Microspheres: In-vitro, Ex-vivo and In-vivo Characterization.

Nicardipine hydrochloride is highly soluble at low pH values. The objective of this investigation was to design, manufacture, and refine the drug’s floating microspheres to increase its bioavailability and prolong its period of residence in the gastrointestinal tract. To optimize the Box-Behken and prepare the floating microspheres, solvent evaporation was employed. The formulation F5 was discovered to be the best as anticipated by the design expert software’s point prediction. Evaluations of pre- and postcompressional parameters were conducted. Utilizing several kinetic models, the drug release pathways were examined. The drugs and excipients did not interact, according to the FTIR/DSC investigations. According to the radiological approach, F5 showed good in-vitro buoyancy. The gastroretentive property of microspheres is revealed by X-ray pictures obtained at 2, 8, and 12 hours for the buoyancy investigation. F5 (235.04%) demonstrated a high relative bioavailability over oral tablets, according to the in-vivo pharmacokinetic investigation. In comparison to the marketed formulation group, the F5-treated group experienced a considerably larger percent decline in BP values (20.00 ± 6.00 and 13.00 ± 4.00%, respectively) at 36 and 48 hours of the in-vivo pharmacodynamic testing. For 90 days, the F5 formulation was maintained at 5 ± 2 and 25 ± 2°C, indicating the stability of nicardipine microspheres.

Development and Characterization of Ethanolic Extract of Cleome gynandra L. Loaded Solid Lipid Nanoparticles for the Management of Diabetes Mellitus

The bioactive components of the botanical remedy Cleome gynandra L., which is famous for its antidiabetic effects, were extracted using ethanol. To improve its stability, bioavailability, and therapeutic potential, the extract was subsequently encapsulated within solid lipid nanoparticles (SLNs) using a high-pressure homogenization method with varying concentrations of lipids. Zeta potential, entrapment efficiency, kinetics of drug release, and particle size were among the numerous characteristics of the SLNs that were thoroughly examined. One important measure for determining whether bioactive compounds were successfully encapsulated within the SLNs is the entrapment efficiency. An impressive entrapment efficiency of more than 82.13% was shown by the optimized formulation F4. The optimized formulation F4 exhibited a mean particle size ranging from 243.5 to 261.7 nm, according to particle size analysis. This size range is ideal for improving cellular uptake and bioavailability. A negative charge was observed in the zeta potential measurements, which means that the SLNs are stable and do not aggregate. A PDI of 0.416 provided additional evidence of the nanoparticles’ stability and uniformity. A sustained release of about 62.57% over 7 hours was shown in the in-vitro drug release profile data, indicating a long-lasting therapeutic effect. Improved therapeutic efficacy of antidiabetic treatment and more stable blood glucose levels are both benefits of the sustained release profile. The in-vitro results of formulation F4 suggest that SLNs have the good stability, bioavailability, and therapeutic potential of C. gynandra L.’s ethanolic extract when used as a delivery system.

Formulation and Evaluation of Nanoparticle Loaded Hydrogel Containing Antifungal Agent for the Treatment of Onychomycosis Using Factorial Design.

SLNs are hopeful carriers for the topical delivery of antifungal drugs. This research aimed to develop a topical gel combining Efinaconazole-loaded SLNs with fluconazole to enhance the treatment of onychomycosis. The objective was to formulate a nail gel that capitalizes on the localized action and improved adherence of efinaconazole, a crucial agent in treating nail disorders like onychomycosis. The formulation utilized an alcohol-based system with specialized ingredients to ensure low surface tension and optimal wetting properties. Fluconazole, a broad-spectrum third-generation triazole antifungal, was included for its systemic and superficial antifungal activity. It works by inhibiting the formation of ergosterol, a key component of fungal cell membranes, by blocking the fungal cytochrome P-450 enzyme. The SLN-based delivery system allows for the slower release of Efinaconazole, while fluconazole diffuses more rapidly. The optimized gel formulation showed sustained drug release, with Efinaconazole releasing 32.85% of the drug by the 8th hour, compared to 74.05% for fluconazole during the same period. A stability study on the F4 formulation, which utilized Carbopol 934, was conducted according to ICH guidelines and demonstrated that the gel maintained its quality attributes, such as color, odor, homogeneity, pH, and viscosity over 6 months of testing. These results indicate that the F4 topical gel formulation is stable and suitable for long-term use.

Development and Analysis of Colon-Specific, pH-Responsive Polymer Delivery of Irinotecan Hydrochloride Tablets for Colon Cancer Treatment.

For the formulation of enteric-coated tablets containing irinotecan hydrochloride, this thesis focuses on HPMC and ethylcellulose, both of which are pH- and oxidation-resistant polymers. The integrated polymer-drug tablet mixture was coated with 15% of eudragit S100 and L100, which is a methacrylic acid copolymers, that’s soluble at pH 7. Both the physical characteristics with the invitro release kinetics pattern of the enteric-coated tablets were characterized. In the invitro release study, different pH environments were used, comparable to the gastrointestinal tract (GIT): 0.1 N HCl solution for two hours, pH 6.8 phosphate buffer for three hours, and pH 7.4 phosphate buffer for six hours. Using this device, you can simulate the pH level of the mouth, the digestive tract, and the urinary tract. As a result of consistent release studies, formulation F7 released 88.2% of the drug after 12 hours. Models such as Higuchi, Korsmeyer-Peppas, and zero-order reactions were used to analyze the GIT. This directed the development of a sustained delivery pattern that may be perfect for colonic IRT administration in the eventual treatment of colon cancer. Among the nine formulations, F7 formulated with EC and HPMC extended best sustained release pattern of drug, hence it is suitable for treating colon cancer.

Design and in vitro Evaluation of Cocoa Butter-based Amlodipine Besylate Fast Melt Tablets

Background: Oral fast-melting tablets (FMTs) have been gaining popularity due to their advantages in resolving swallowing issues of conventional oral tablets. Cocoa butter is an excipient of choice to develop FMT with an acceptable taste and faster onset of action of the drug. Purpose: The present study aimed to prepare and characterize the amlodipine besylate-loaded cocoa butter FMTs. objective: To prepare and characterise the formulation of cocoa butter tablet as fast melt buccal delivery system of amlodipine besylate. Method: Amlodipine besylate FMTs were prepared using a simple freezing (refrigeration) method. Cocoa butter (Form V) was used as the base to achieve a final tablet weight of 500 mg with drug and other functional excipients. The designed prototype tablet formulations were subjected to disintegration tests to determine the robust selected batch. The formulation F4, containing 7% high-molecular-weight chitosan, exhibited the quickest disintegration time of 1.45 ± 0.10 min. Afterwards, the selected formulation, F4, was subjected to quality evaluation parameters. Results: Fourier transform infrared spectroscopy (FTIR) studies revealed that there was no incompatibility between amlodipine besylate, cocoa butter, and other excipients. The average hardness of the F4 formulation tablet batch was found to be 2.69 ± 0.21 kg/cm2 and a friability of less than 1%. The drug content in F4 tablets was found to be 102.38 ± 5.29% and showed an in-vitro drug release of 94.30 ± 2.63% within 30 min. Over a six-month stability testing period, the chosen F4 formulation did not significantly change in terms of tablet average weight, disintegration time, drug content, and in-vitro dissolution rate. Conclusions: Selected formulation F4 with 7% of high molecular weight chitosan exhibited good physical properties, indicating the suitability of cocoa butter as a base to produce FMTs with the aid of a natural super-disintegrant.

Preparation and Evaluation of Itraconazole Nanoparticle Lipid Carrier Gel for Dermatophytosis

Fungal infection is one of the common dermatological diseases. Drug delivery systems for topical use have shown significant advantages in targeting the drug to the action site in the body and also reduces the systemic side effects. Itraconazole was chosen as a model drug with low aqueous solubility. In the present study an attempt was made to prepare itraconazole loaded nanostructured lipid carrier (NLC). Different formulations were prepared by hot homogenization technique using solid lipid and liquid lipid (Compritol 888 &amp; Caprol PGE 860) and surfactants (Poloxamer 188, tween 80). All the Formulations were characterized for drug content, entrapment efficiency, particle size, poly dispersity index, zeta potential &amp;in vitro drug release and FTIR was done to study any interaction between excipients. The best formulation shows better drug release and entrapment efficiency 83.2%. the best formulation F3 showed better in-vitro drug release 55.46% at the end of 8th hour. The F3 was made into gel using Carbopol as a gelling agent. SEM study revealed that the NLC gel shows the particle size was found to be 500 nm in size smooth surfaces. NLC gel shows Drug release of NLC gel followed non- Fickian diffusion. NLC gel were stable at 40 ± 2ֹ°C and 75 ± 5% RH. Thus, the prepared NLC gel proved to be a potential candidate as a topical nanoparticulate sustained drug delivery system for itraconazole (BCS class II drug). keywords: Itraconazole, Nanoparticle Lipid Carrier, Lipids.

Optimizing locally delivered periodontitis therapy: Development of chitosan‐hydroxyapatite‐encapsulated drug via electrospraying

AbstractThis study presents the development of an optimized drug delivery system for periodontitis treatment utilizing chitosan‐hydroxyapatite nanoparticles. Employing the electrospraying technique, researchers encapsulated the antibiotic amoxicillin within chitosan‐hydroxyapatite composite matrices while varying the concentrations of chitosan and hydroxyapatite nanoparticles. The resulting microparticles displayed sizes ranging from 276 to 386 μm. Characterization of the produced drug encapsulations indicated that higher concentrations of chitosan and hydroxyapatite resulted in the formation of larger particles with rougher surfaces, increased mechanical strength, and enhanced thermal stability. Notably, nanoindentation analysis revealed an increase in hardness from 0.21 to 0.35 GPa, and in elastic modulus from 5.32 to 8.72 GPa with escalating chitosan and hydroxyapatite content, meeting or surpassing requirements for load‐bearing regenerative biomaterials. In vitro drug release assessments exhibited sustained amoxicillin release over 24 h, predominantly through diffusion and dissolution mechanisms. Formulations with lower polymer and mineral content showcased elevated release rates, with the F1 encapsulation (0.5% chitosan, 0.2% HAP) achieving a cumulative release of 78.3 ± 3.2% in contrast to 65.1 ± 2.7% for the F5 formulation (2.5% chitosan, 1% HAP). These encapsulations selectively modulated the overproduction of proinflammatory cytokines, including IL‐1β, IL‐6, and TNF‐α, in gingival fibroblasts and osteoblasts without compromising cell viability. An artificial neural network (ANN) model accurately forecasted the material properties and biological performance of the formulations based on their compositional variations, yielding correlation coefficients exceeding 0.97. This computational platform offers a virtual screening tool for refining regenerative and drug delivery therapies. The developed chitosan‐hydroxyapatite microparticulate system demonstrates promising potential for prolonged treatment of periodontitis through controlled antibiotic delivery, improved mechanical properties, and targeted regulation of the inflammatory response.

Formulation and Evaluation of Tamsulosin Hydrochloride Sustained Release Capsules Using Pelletization Technique

Tamsulosin HCl is an αq-1 adrenergic receptor antagonist that is primarily used to treat benign prostatic hyperplasia (BPH), a disease defined by an enlarged prostate. The aim of this project is to develop, analyze, and compare the developed formulations to the innovator product (Flomax). The formulations were prepared by integrating Eudragit L100-55 as enteric polymers in various formulations, Drug coat L30D as a sustained release coating polymer, and PEG 6000 as pore forming in distinct quantities. The formulation F8 exhibited %CDR of 98.8%, comparable to the Flomax (innovator product) and the similarity factor (f2) was calculated and found to be 94.3% marking this formulation equivalent to the innovate product. The improved formulation was tested for stability for the 1st month at 40 ± 2°C and 75 ± 5% R_H, as per ICH guidelines. The regression results of the improved formulation led to an inference that F8 indicates first-order kinetics with an estimated regression value of 0.926, and it was concluded that the drug had been released through diffusion mechanism.