Topical Dosage Forms Research Articles

Spectrometric method for simultaneous quantification of nadifloxacin and salicylic acid in a novel topical dosage form

Acne vulgaris is a prevalent skin disorder that affects many individuals. In the search for effective acne therapy, researchers have found that a combination of Nadifloxacin and Salicylic Acid may produce a synergistic effect. To further investigate this, a study was conducted to devise a spectrophotometric method for simultaneously measuring the concentrations of Nadifloxacin and Salicylic Acid in a novel topical formulation. Simultaneous Estimation Method was employed using methanol as the solvent. Nadifloxacin exhibited an absorbance maximum of 291 nm, while Salicylic Acid showed an absorbance maximum of 297 nm in methanol. Linearity experiments were conducted to determine the concentration ranges for both drugs, which were found to be 2–12 ppm for Nadifloxacin and 5–30 ppm for Salicylic Acid. The recovery results of Nadifloxacin ranged from 82 % to 95 %, while those of Salicylic Acid ranged from 97 % to 110 %. These results indicate the accuracy and reliability of the method. This method was further validated in accordance with the guidelines provided by the International Council for Harmonization (ICH) of Technical Requirements for Human Use. The proposed method has demonstrated its applicability for the simultaneous and quantitative assessment of Nadifloxacin and Salicylic Acid in various dosage forms. This development is significant as it provides a reliable and efficient means of measuring the concentrations of these two drugs in acne therapy formulations.

Synthetic membrane selection for in vitro release testing (IVRT): A case study of topical mometasone furoate semi-solid dosage forms

In vitro release testing (IVRT) is extensively used to develop the formulation of topical semi-solid products, to evaluate the quality and consistency of the product after scale-up and post-approval changes, and more recently to aid the evaluation of topical generic products’ equivalency. The selection of synthetic membrane is one of the most critical parameters of the method development part of IVRT. It is well known that the membrane features namely its polymer matrices, porosity, pore size, thickness can have a substantial effect on the IVRT data. However, there is no detailed information available in the literature regarding the membrane selection for different types of topical dosage forms. Therefore, we aimed to investigate whether difference topical semi-solid dosage forms of the same drug molecule would cause to variation in the membrane selection. Within this framework, rheological behaviour of commercially available three different types of topical semi-solid dosage forms (ointment, cream, and lotion) of mometasone furoate (0.1%) were primarily characterized. Then, the membrane inertness test was conducted using a series of synthetic hydrophilic membranes (regenerated cellulose, cellulose acetate, cellulose nitrate, mixed cellulose ester membranes) and hydrophobic membranes (polyether sulfone, polypropylene, polytetrafluoroethylene membranes) after identifying of an appropriate receptor medium that ensures sink condition for mometasone furoate. Lastly, IVRT studies from the topical semi-solid products were performed utilizing Franz-type diffusion cells. The membrane inertness and in vitro release data demonstrated that the cellulose acetate membrane showed superior diffusion properties in general while the other synthetic membranes exhibited varying outcomes for different semi-solid dosage forms of mometasone furoate. Overall, the results indicated that the release rate and the cumulative drug released amount of drug after 6 h through the different synthetic membranes might vary depending on the semi-solid dosage form. In order to select the synthetic membrane for IVRT, it should also be considered potential interactions between the polymer matrices and the chemical structure of drug molecule as well as formulation components prior to conducting membrane inertness test and IVRT studies.

Relieving postherpetic neuralgia pain via gabapentin-loaded bigels as an auspicious topical drug delivery system.

Over the past decades, a substantial portion of the population worldwide has been infected with varicella zoster and most cases developed shingles. Unfortunately, shingles is usually accompanied by postherpetic neuralgia, which may persist for months to years after the resolution of the viral infection. Gabapentin is an orallygamma-aminobutyric acid analogue approved by the Food and Drug Administration to manage shingles postherpetic neuralgia. However, gabapentin shows nonlinear pharmacokinetics, with variable absorption and bioavailability along with its short half-life and long side effects that may include dizziness and somnolence, which calls for an appropriate topical dosage form. Bigels are unique semisolid dosage forms with boosted penetrability and satisfactory hydrophilic texture. The current work pointed to formulating gabapentin-loaded bigels for the treatment of postherpetic neuralgia, where the analysis and optimization of design were performed via Design-Expert®. The selected bigel (F5), incorporating 400mg Span 60, 1000mg Tween 80, and 1000mg Transcutol, displayed spherical nanosized particles with acceptable viscosity and spreadability. Subsequent topical application of the selected bigel on the skin of Wistar rats, F5, demonstrated a boosted accumulation of gabapentin in the skin similar to PLO gel but superior to the drug solution. Furthermore, a histopathological study demonstrated the biosafety of the selected bigel when applied topically. Accordingly, gabapentin-loaded bigel would be considered a potentially topical dosage form for the delivery of gabapentin for the management of postherpetic neuralgia.

Betulin-NLC-hydrogel for the Treatment of Psoriasis-like Skin Inflammation: Optimization, Characterisation, and In vitro and In vivo Evaluation.

Psoriasis is a chronic inflammatory skin disorder that poses significant challenges regarding effective and targeted drug delivery. Bioactive substances like betulin have shown tremendous utility in treating these conditions; however, they pose limited utility owing to their physicochemical characteristics. Here, we aimed to develop a novel topical dosage form for treating psoriasis, utilising betulin-loaded solid lipid nanoparticles (NLCs) incorporated into a hydrogel matrix. The optimization of the formulation was meticulously conducted using a design of experiments methodology, and its diverse physicochemical attributes were thoroughly examined. Evaluating betulin's in vitro release pattern from the NLC-hydrogel demonstrated consistent and regulated drug release properties. Additionally, the formulation demonstrated improved skin penetration abilities as determined by in vitro skin permeation experiments employing Franz diffusion cells- furthermore, the therapeutic effectiveness of the betulin-NLC-hydrogel was assessed by an in vivo experiment carried out using an imiquimod-induced psoriasis-like skin inflammation model in BALB/c female mice. The NLCs exhibited a pH of 5.67±0.86, particle size of 148.16±12.66 nm, and zeta potential of -22.84±2.37 mV, ensuring stability and suitability for topical use. The gel, with a pH of 6.05±0.43 and viscosity of 17550±120 cPs, showed enhanced skin hydration and lipid restoration. Drug release studies indicated a slower release from NLCs and gel, improving skin retention. Stability tests revealed that the formulations were stable at room temperature but not at elevated temperatures. The in vitro safety profile of the formulation revealed no significant adverse effects on HaCaT cell lines. The NLC gel demonstrated significant anti-psoriatic activity, reducing inflammation and cytokine levels. The betulin-NLC-hydrogel formulation exhibited promising characteristics for the topical treatment of psoriasis, showcasing optimised drug delivery, sustained release, and notable therapeutic efficacy. The findings from this study provide a foundation for the potential clinical translation of this innovative topical dosage form for improved psoriasis management.

Teriflunomide Transdermal Cream: In-vitro And In-vivo Evaluation for the Treatment of Rheumatoid Arthritis.

Rheumatoid Arthritis (RA) is an incurable long-term disease that requires continuous safe treatment. Currently, many antiinflammatory agents and steroids are used to manage the diseases and are associated with a variety of side effects. There is a great need for a formulation that addresses the root cause of the disease and can be used for prolonged periods without any side effects. Hence, an attempt was made to develop a formulation of an alternative to steroid formulations that can be used for prolonged periods without/minimal side effects, i.e., teriflunomide topical dosage form. Teriflunomide tablet was approved for multiple sclerosis. It is the primary metabolite of leflunomide which is approved to treat RA. When leflunomide is administered orally converts to teriflunomide to elicit its action as such, leflunomide has no anti-rheumatoid effect. Both leflunomide and teriflunomide have different GIT side effects such as diarrhea, nausea, and hepatotoxicity on oral administration. To avoid these oral side effects of leflunomide and teriflunomide and to improve RA treatment compliance, teriflunomide was formulated as a topical cream. The developed topical cream is designed to be applied at night on the affected joints. It is intended to release the drug during the night, provide higher localized concentrations of the drug in the synovial joint and reduce GI and systemic side effects improving treatment compliance.

Algorithms for topical therapy of mycoses at the daily appointment of a dermatologist

This article discusses the immediacy of the problem of rising incidence of common mycoses that dermatovenerologists deal with at outpatient visits, the reasons for their occurrence, conversion from one course of the disease to another and the use of etiological effective treatments. The author described the mechanisms of development of different mycoses according to their etiology, comorbid disorders accompanying mycoses and the features of the clinical picture based on etiological factors and sites of infection. The article places special emphasis on the reasons for infection with fungal invasions in humans, conditions and numerous contact routes. Modern features of the course of fungal skin diseases include formation of biofilms in the sites of infection, multicentricity, extension of the pathological process, frequent formation of granulomas, follicles, occurrence of numerous mycoides, as well as the low virulence of dermatophytes. The publication also presents various clinical cases of somatically healthy patients suffering from various mycoses caused by variant factors, which have pathological processes located in different sites. According to the doctor’s prescription, patients used conventional treatment regimens that included external/ topical treatment and general therapy, strictly in accordance with clinical guidelines – the use of highly active broad-spectrum antifungal drugs with fungicidal, fungistatic, antibacterial, anti-inflammatory and antipruritic action. These properties ensure a low probability resistance of microorganisms or relapses during treatment with topical dosage forms of antifungal drugs for cutaneous application. Upon completion of the course of treatment, patients reported a significant improvement in their skin condition resulting in minimization of disease symptoms, disappearance of skin rashes, skin itching, and elimination of exfoliation.

Development and Validation of Reversed-phase High-performance Liquid Chromatography Method for Simultaneous Estimation of Desonide and Curcumin in Topical Dosage Form

Development and Validation of Reversed-phase High-performance Liquid Chromatography Method for Simultaneous Estimation of Desonide and Curcumin in Topical Dosage Form

Stability-indicating liquid chromatographic method development and validation for quantification of trifarotene in pure and topical drug product

BackgroundTrifarotene is effective for treating acne and other skin issues. To ensure its quality and meet regulatory standards, a reverse phase liquid chromatography (RP-LC) stability-indicating method was developed and validated for its quantification in pure and topical dosage forms. An isocratic elution chromatographic method was employed, using an octadecylsilyl silica gel-packed column (150 mm × 4.6 mm, 3 µm particle size). The mobile phase was a mixture of phosphate buffer and acetonitrile (40:60 v/v). Chromatographic conditions included a flow rate of 0.5 mL/min, column temperature of 40 °C, detection at 265 nm, and injection volume of 20 µL.ResultsThe developed analytical method reports the retention time of trifarotene 11.2 min, higher theoretical plate count, asymmetric peak, and good resolution between the peaks of trifarotene, phenoxyethanol, and environmentally generated impurities.ConclusionThe analytical method has been found to be linear, accurate, robust, specific, and selective for impurities produced during forced degradation studies. The proposed analytical method can be utilized for routine pharmaceutical analysis of trifarotene to judge its quality and safety.

Formulation and Evaluation of Nicotinamide Microsponges – The First Step Towards the Development of a Novel Topical Dosage Form

The objective of this work was to formulate and analyze microsponges of nicotinamide. The said formulation was created using the emulsion solvent diffusion technique, and a 3 level two factor-based factorial design was applied to optimize the effect of the stabilizer (X1), as well as drug (X2), amounts on the entrapment efficiency (Y1) and average particle size (Y2). Various parameters, such as flow characteristics, percentage yield, drug concentration, in-vitro drug release tests, entrapment efficiency, and scanning electron microscopy (SEM), were evaluated. All parameters were found to be within the acceptable range. Design Expert 13 was employed to optimize the microsponges, and the optimal batch was determined by examining the desirability data. From this analysis, the optimal amounts of drug and stabilizer were found to be 302.87 and 59.71 mg, respectively. The reliability of the preparation and evaluation of the optimized batch was confirmed by a less than 5% discrepancy between the observed and predicted values of parameters. SEM images revealed that the microsponges were prepared with uniform and spherical morphology. The study concluded that nicotinamide microsponges were successfully prepared and evaluated. Further steps will involve incorporating this formulation into a novel topical dosage form.

Assessment of Wound Healing Potential of Simvastatin Emulgel in Rat Excision Wound Model

Background: Microorganisms can infect wounds and disrupt healing by causing inflammation and tissue injury Objective: Simvastatin (SIM) is reported to have antibacterial activity; therefore, this research is designed to evaluate the efficacy of simvastatin emulgel in wound healing. Methods: The simvastatin emulgel was assessed for physical appearance, rheological behaviour, spreadability, pH, ex vivo drug release and in vivo activity. The wound-healing activity was assessed by percent wound contraction, hydroxyproline estimation and histopathological evidence in wound-induced albino rats. Results: The simvastatin emulgel exhibited viscosity and spreadability of 6875 ± 531.21 mPa.s and 10.15 ± 0.31 g.cm/sec, respectively. The simvastatin emulgel exhibited wound contraction in wound healing studies compared to the reference product (p < 0.05). This activity was statistically significant (p < 0.05) in comparison to the control. The hydroxyproline content supported the wound-healing promoting effect of simvastatin emulgel, and marked improvements in the skin histological architecture were seen in the histopathological study. Conclusion: The study manifested the promising potential of simvastatin emulgel in speeding the healing of rat wounds with epithelization. Therefore, the designed simvastatin emulgel can be used as an option for the conventional topical dosage form.

A Derivative Spectrophotometric Method for the Vierordt’s Detection of Terbinafine and Itraconazole in Topical Dosage Form

The goal of the current work was to simultaneously estimate the dosage forms of pharmaceutical topical dosage form and bulk itraconazole and terbinafine HCl by developing and validating a novel and straight forward UV spectrophotometric approach. As of right now, no reports of this medication combination for simultaneous UV spectrophotometric analysis exist. Acetonitrile was utilized as a solvent in the UV Shimadzu 1800 model, which was employed to test the developed approach. For Terbinafine HCl, the wavelength at which the λmax was measured was 235 nm, while for itraconazole, it was 263 nm. It was discovered that the percent RSD of both the system and technique precision for itraconazole and terbinafine HCl was less than 2%. In summary, a new and straightforward UV spectrophotometric technique was created and verified for the simultaneous measurement of terbinafine HCl and itraconazole in pharmaceutical topical dosage form and bulk dose forms. The created approach was determined to be precise, accurate, linear, and stable because the results were found to be within the given range. KEYWORDS Itraconazole, Terbinafine HCl, UV spectrophotometric, Validation, Simultaneous estimation method, vierordt’s method

Microemulsion-Based Polymer Gels with Ketoprofen and Menthol: Physicochemical Properties and Drug Release Studies.

Ketoprofen is a non-steroidal, anti-inflammatory drug frequently incorporated in topical dosage forms which are an interesting alternatives for oral formulations. However, due to the physiological barrier function of skin, topical formulations may require some approaches to improve drug permeation across the skin. In this study, ketoprofen-loaded microemulsion-based gels with the addition of menthol, commonly known for absorption-enhancing activity in dermal products, were investigated. The main objective of this study was to analyze the physicochemical properties of the obtained gels in terms of topical application and to investigate the correlation between the gel composition and its mechanical properties and the drug release process. Microemulsion composition was selected with the use of a pseudoternary plot and the selected systems were tested for electrical conductivity, viscosity, pH, and particle diameter. The polymer gels obtained with Carbopol® EZ-3 were subjected to rheological and textural studies, as well as the drug release experiment. The obtained results indicate that the presence of ketoprofen slightly decreased yield stress values. A stronger effect was exerted by menthol presence, even though it was independent of menthol concentration. A similar tendency was seen for hardness and adhesiveness, as tested in texture profile analysis. Sample cohesiveness and the drug release rate were independent of the gel composition.

Evaluation of drug release from topical dosage forms and permeability prediction through the skin barrier (review)

Introduction. The review considered the basic concepts of drug release and kinetic modeling of this process from dosage forms (DF) according to the dissolution profile using a vertical Franz diffusion cell.Text. Drug release from dosage forms (ointments, gels, transdermal patches and polymer films) is usually described as the processes of drug dissolution in the biological system. Formally, this process, in accordance with pharmacopoeial methods, is assessed using various solubility tests. The theoretical aspects of drug release are based on the theory of mass transfer of substances from a polymer matrix into a system that simulates a biological environment. Drug release can be carried out via the passive diffusion mechanism according to Fick and "non-Fick" diffusion, drug desorption from the inner side of the membrane, as well as other mechanisms. Drug release is determined both lipophilicity and the membrane nature, both various physicochemical parameters of the drug. One of the correlation characteristics of mass transfer is the assessment of the permeability coefficient for a specific membrane that simulates skin. Permeability coefficient describes the rate of penetration of a drug per unit concentration in distance/time units. An example of relationship of "structure-permeability" correlation are the equations relating the permeability constant and lipophilicity to the molecular weight of the drug. The paper showed statistical methods of data analysis (MANOVA, ANOVA) and model-dependent methods (zero order, first order, Higuchi model, Korsmeyer – Peppas model, Hixson – Crowell model, etc.). The ideal drug delivery of non-degradable and non-disaggregating drugs describes as drug release model by zero-order reaction. For drug release of water-soluble drugs from a porous matrix, first-order reaction model is more typical. Kinetic models of fractional power functions are used usually as the cube root law (Hixson – Crowell model) or the square root law (Higuchi model) to describe the process of drug release from gels and dermal films and patches. The Korsmeyer – Peppas model allows us to evaluate the mechanism of mass transfer with Fickian diffusion or another process.Conclusion. Mathematical modeling of the drug release kinetics from soft dosage forms is an important element for the development and optimization of their compositions. The study of the drugs release from soft dosage forms, including TTS and polymer films, as well as the release from solid dosage forms, is based on establishing correlations between the kinetics of the release and dissolution profile. The main release models, regardless of the DF, remain the following models: zero order, first order, Korsmeyer – Peppas, Higuchi, Hickson – Crowell, the empirical or semi-empirical constants of which vary significantly depending on the DF and the release mechanism (Fickian diffusion or another drug mass transfer mechanism). Correlation relationships QSPeR or QSPR, using the coefficients of permeability, diffusion and lipophilicity, provide information on the mass transfer of drugs through the skin.

Formulation and Characterisation of Fluconazole Loaded MCM-41 Powder for Topical Drug Delivery

Purpose: The use of common carriers like talc for topical drug delivery leads to diminished efficacy as a result of poor aqueous solubility and low dissolution rate. The objective of this study was to improve the efficiency of fluconazole topical dosage form using MCM-41 as a carrier material. The aim was to load fluconazole in carriers like MCM-41 as well as ß-Cyclodextrin and to compare the prepared powder formulation with the marketed formulations. Methods: Fluconazole complex was formulated with the use of MCM-41 and ß-CD as carriers in different proportions by melt, solvent evaporation and kneading method. The complex was developed into a powder formulation. These formulations were subjected to in vitro anti-fungal activity tests on candida albicans. Results: The inclusion compound was characterised by X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and FTIR. The optimised method of preparation determined by in vitro dissolution was the melt method. The optimised formulation was then subjected to anti-fungal activity test. Formulation B containing MCM-41 as the bulk excipient had better performance than the marketed formulation; it showed 92.95 ± 0.33% CDR compared to 74.96 ± 0.47% CDR at the end of 1 hour and increased moisture adsorption. Conclusion: Thus, a fluconazole topical formulation with improved drug dissolution and moisture adsorption was designed. From in vitro tests, it was seen that the prepared formulation had better performance compared to the commercial formulation against skin mycotic infections and could be used for its treatment.

Formulation study of PLGA in situ films for topical delivery of salicylates

A film-forming system (FFS) represents a convenient topical dosage form for drug delivery. In this study, a non-commercial poly(lactic-co-glycolic acid) (PLGA) was chosen to formulate an FFS containing salicylic acid (SA) and methyl salicylate (MS). This unique combination is advantageous from a therapeutic point of view, as it enabled modified salicylate release. It is beneficial from a technological perspective too, because it improved thermal, rheological, and adhesive properties of the in situ film. DSC revealed complete dissolution of SA and good miscibility of MS with the polymer. MS also ensures optimal viscoelastic and adhesive properties of the film, leading to prolonged and sustained drug release. The hydrolysis of MS to active SA was very slow at skin pH 5.5, but it apparently occurred at physiological pH 7.4. The film structure is homogeneous without cracks, unlike some commercial preparations. The dissolution study of salicylates revealed different courses in their release and the influence of MS concentration in the film. The formulated PLGA-based FFS containing 5 % SA and 10 % MS is promising for sustained and prolonged local delivery of salicylates, used mainly for keratolytic and anti-inflammatory actions and pain relief.

Exploring the Therapeutic Potential of Vesicular Nanocarrier Systems for Elimination of Skin Cancer

Background:: Skin cancer, a common malignancy worldwide, has increased incidence and mortality. Thus, it is a public health issue and a significant illness burden, which increases treatment costs. Chemotherapy and surgery are used to treat skin cancer. However, conventional skin cancer treatments have several limitations, demanding the development of innovative, safe, and effective methods. To overcome these limitations of conventional topical dosage forms, many nanocarriers have been developed and tested for the targeted delivery of anticancer drugs. Objective:: The main objective of the present review was to discuss the utility of various vesicular nanocarrier systems to deliver anticancer drugs following topical administration to treat skin cancer. Methods:: For this review article, we scoured the scholarly literature using Science Direct, Google Scholar, and Pubmed. Discussion:: The vesicular drug delivery system has been intensively explored and developed as an alternative to conventional skin cancer drug delivery systems, especially for melanoma. They improve the penetration of anticancer drugs via the skin, reaching the cancer area with enough and killing cancer cells. Vesicles minimize skin irritation and drug degradation. This improves therapy efficacy and reduces systemic toxicity. Conclusion:: Utilizing the vesicular drug delivery system shows promise in treating skin cancer. Therefore, further research and inquiries are necessary to explore the therapeutic potential of these substances in treating skin cancer, intending to develop a personalized, efficient, and secure therapy approach for patients with this condition.

Clinical Assessment of Topical Methotrexate Micro-emulsion as a Treatment for Psoriasis: A Randomized Clinical Trial

Objectives: Psoriasis is an inflammatory skin disease, and the main topical treatment for this disease is corticosteroids, vitamin D analogs, salicylic acid, and calcineurin inhibitors. This study clinically evaluates a topical dosage form of methotrexate (MTX) micro-emulsion and compares it with clobetasol lotion. Methods: The employed methodology involves 20 patients with symmetric psoriasis. Topical MTX micro-emulsion (0.25%) was used on one side and clobetasol lotion (0.05%) on the other side. The psoriasis area and severity index score were used to evaluate the results in weeks 0, 4 and 8. Results: The average psoriasis improvement and psoriasis area and severity index score reduction using topical MTX micro-emulsion were 47.24%±10.1524% and 73.5%±6.34% at the end of the first and second months of treatment. The results using clobetasol lotion were 56.5%±8.08% and 73.4%±7.27% after the first and second months of treatment, respectively. There was a significant statistical difference between MTX micro-emulsion and clobetasol lotion after the first month of treatment (α=0.005); however, this difference was not significant after the second month (α=0.938). Discussion: The application of topical MTX micro-emulsion can be effective in improving psoriasis and is much safer compared to injectable forms.

Formulation and Characterization of Double Emulsions W/O/W Stabilized by Two Natural Polymers with Two Manufacturing Processes (Comparative Study)

Four distinct types of multiple emulsions were synthesized using xanthan gum and pectin through two distinct manufacturing processes. The assessment encompassed the examination of morphology, stability, and rheological properties for the resulting water-in-oil-in-water (W/O/W) double emulsions. Formulations were meticulously crafted with emulsifiers that were compatible with varying compositions. Remarkably stable multiple emulsions were achieved with a 0.5 wt% xanthan concentration, demonstrating resilience for nearly two months across diverse storage temperatures. In contrast, multiple emulsions formulated with a higher pectin concentration (2.75 wt%) exhibited instability within a mere three days. All multiple emulsions displayed shear-thinning behavior, characterized by a decline in apparent viscosity with escalating shear rates. Comparatively, multiple emulsions incorporating xanthan gum showcased elevated viscosity at low shear rates in contrast to those formulated with pectin. These results underscore the pivotal role of the stepwise process over the direct approach and emphasize the direct correlation between biopolymer concentration and emulsion stability. This present investigation demonstrated the potential use of pectin and xanthan gum as stabilizers of multiple emulsions with potential application in the pharmaceutical industry for the formulation of topical dosage forms.

Nano Sponge: An Emerging Nano-Technology Based Drug Delivery System

In current scenario medical experts have long struggled with how to deliver medication to targeted location into the body while also controlling the drug release rate to avoid overdosing. This issue may be resolve through the creation of novel, intricate formulation known as nano sponges. Nano sponges are small sponge, all around size virus, that may hold a range of medication. These microscopic sponges can move through the system until they reach the intended target region, where they adhere to surface and start to release the drug in steady and controlled manner. Nano sponges are a network or 3D polyester scaffold that are spontaneously decompose. These polyesters are combined with cross-linkers agent in a solution to create a nano sponge. When loaded nano sponge’s framework breakdown the drug particle is released. They are mostly in solid form and it can be formulated as oral, parenteral, topical, or inhalation dosage form, several studies havebeen conducted on protein, peptide, genes, anti-cancer biomolecules via nano-particle technology which hep to reduce undesirable effect and enhance efficacy.

Hydrotrope dynamics: unraveling solubility pattern and correlation of benzimidazole using response surface methodology expert system

Solubilizing drugs in liquid and semisolid environments typically involves the use of cosolvents or surfactants. In contrast, the utilization of hydrotropic agents, which are small hydrophilic organic compounds like sodium salicylate or sodium benzoate, has been less explored in the field of pharmaceutical formulations. However, particularly in the context of topical dosage forms, hydrotropic solubilization can present valuable alternatives for enhancing solubility. One challenge in employing hydrotropic solubilization has been the unpredictability of its effectiveness with different drug molecules. In the current study, three different hydrotropes namely sodium salicylate, sodium benzoate, and pyrogallol were chosen to test the solubility enhancement of benzimidazole drug. Optimization of solubility was proceeded with Central Composite Design obtained from RSM expert system. It was noticed from the results that sodium salicylate had performed the best compared to the other two chosen hydrotropes. This was also reexamined using two models namely modified Apelblat model and polynomial model. The thermodynamic studies were assessed and it had reconfirmed the acquired solubility study results. The minimum and maximum hydrotrope concentrations of sodium salicylate required were 0.4 and 2.25 mol/L, respectively. The solubility enhancement factor was also remarkably high for sodium salicylate with 36.91 ± 0.07. With careful selection of the appropriate hydrotropic agent, the solubility of poorly soluble drug, benzimidazole has been significantly improved.