Drug Content Analysis Research Articles

Dexamethasone-loaded PLGA porous microspheres used as 3D-bioprinted bioink promote tissue-engineered cartilage regeneration

The current investigation focused on fabricating and thoroughly analyzing porous microspheres (MPs) comprising poly (lactic-co-glycolic acid, PLGA) encapsulating dexamethasone, by utilizing the water-in-oil-in-water (W/O/W) emulsion solvent evaporation technique. The meticulous characterization encompassed various parameters, including particle size distribution, morphology, and polymer integrity, all of which exhibited consistent attributes across the MPs populations. The analysis of drug content and release kinetics revealed a sustained and controlled liberation of dexamethasone, characterized by an initial burst release within the initial 3 days followed by a gradual, protracted release profile. Subsequent in vivo assessments further validated the potent anti-inflammatory effects of the dexamethasone-loaded PLGA MPs, as evidenced by notable reductions in CD86 immunohistochemical staining intensity, along with the change in membrane thickness. Additionally, the MPs demonstrated an impressive capability to support the maintenance of cartilage phenotype, as indicated by the augmented secretion of cartilage matrix components and elevated glycosaminoglycan content.  

Fabrication of lornoxicam loaded into curcumin reinforced nanoemulgel: In-vitro characterization and in-vivo anti-inflammatory potential

Current research aimed to fabricate and characterize lornoxicam-curcumin (LRX-CUR) co-loaded nanoemulgel (NEG) for transdermal delivery. Nanoemulgel was prepared by emulsification method using high sheared homogenization. The prepared NEG was subjected to physicochemical characterizations including thermodynamic analysis, FTIR, pH, drug content, zeta analysis (size distribution, PDI, zeta potential), rheological behavior, spreadability, in vitro drug release, and ex vivo permeation analysis. In vivo anti-inflammatory effects were assessed in experimental animals (in albino rats) using carrageenan for inducing paw edema. The NEG showed optimum and acceptable thermodynamic stability. No phase separation was observed. The pH was acceptable for use on human skin as its range was 5.5–6.5. In drug content analysis, 95.52 ± 5.63 % of LRX and 93.47 ± 8.53 % of CUR were obtained which were in official limit of USP i.e. 100 ± 10 %. No interactions and incompatibility were found between the drugs and NEG components after FTIR analysis. The viscosity and spreadability were optimum for topical application. The LRX-CUR nanoemulsion exhibited droplet size of 215.6 ± 7.89, PDI 0.219 ± 0.03 and zeta potential −12.0 ± 6.41. The LRX-CUR NEG released 85.69 ± 3.54 % of LRX and 86.89 ± 3.34 % of CUR. The permeation of LRX and CUR was 79.43 ± 5.54 % and 83.96 ± 6.21 respectively after 12 h. The optimized LRX-CUR NEG formulation significantly (p < 0.05; ANOVA) inhibited the paw edema in experimental animals as compared to the control and standard groups. Thus, LRX-CUR nanoemulgel formulation can serve as an effective substitute to the oral administration.

Formulation Development and Evaluation of Polyherbal Emulgel for Anti Inflammatory Activity

This study focuses on the formulation development and evaluation of a polyherbal emulgel incorporating curcumin and coriander seed oil, aimed at enhancing anti-inflammatory activity. Preformulation studies were conducted to characterize the physical, chemical, and mechanical properties of the active substances, and to establish a robust basis for the formulation approach. Various parameters including solubility, melting point, partition coefficient, and drug-excipient interactions were assessed to ensure compatibility and efficacy. The emulgel was prepared through a systematic process involving the preparation of a gel base, oil phase, aqueous phase, and subsequent emulsification. The final product was evaluated for various properties such as physical appearance, homogeneity, pH, spreadability, extrudability, swelling index, viscosity, drug content, and in vitro drug diffusion. Stability studies were also conducted over three months to ensure the longevity and reliability of the formulation. Results indicated that the formulated emulgel exhibited desirable physical properties, optimal pH, high spreadability, good extrudability, and a significant swelling index. Viscosity measurements confirmed appropriate consistency, while drug content analysis ensured accurate dosing. In vitro drug release studies demonstrated sustained release profiles, fitting well with kinetic models. Additionally, in vivo anti-inflammatory activity was assessed using a carrageenan-induced paw edema model in rats, showing promising results with notable inhibition of inflammation. Overall, the polyherbal emulgel formulation developed in this study offers a promising alternative for anti-inflammatory therapy, combining the therapeutic benefits of curcumin and coriander seed oil in a stable and effective dosage form. Further studies are recommended to explore clinical efficacy and potential applications in broader therapeutic areas

Extraction, characterisation and evaluation of curcumin gel

This paper describes the formulation and evaluation of transdermal gels for topical delivery of Curcumin. A polymer with well-defined transdermal characteristics, such as Carbopol 934, was used in this investigation. Using a variety of absorption enhancers, including Mannitol, sodium lauryl sulfate, and polyethylene glycol, carbopol, HPMC gels containing 1% curcumin were prepared using a cold technique. Due to its poor bioavailability, Curcumin has been produced in a gel form with sodium lauryl sulfate, mannitol, and polyethylene glycol as absorption enhancers. The gels underwent investigation concerning gelation temperature, pH, viscosity, drug release profile, drug content, stability studies, and kinetic analysis of drug release data. Because sodium lauryl sulfate shows a higher percentage of drug release than other absorption enhancers, it was determined to be a better enhancer of absorption.

Investigating the Presence of Falsified and Poor-Quality Fixed-Dose Combination Artemether-Lumefantrine Pharmaceutical Dosage Forms in Kumasi, Ghana.

Artemether-lumefantrine (AL) is a highly effective and commonly used Artemisinin-based Combination Therapy (ACT) for treating uncomplicated malaria caused by Plasmodium falciparum, including drug-resistant strains. However, ineffective regulatory systems in resource-limited settings can lead to the infiltration of poor-quality and counterfeit antimalarial medicines into the pharmaceutical supply chain, causing treatment failures, prolonged illness, and disease progression. The objective of the study was to assess the quality of selected brands of fixed-dose combination (FDC) AL tablets and suspensions marketed in Kumasi, Ghana. A total of fourteen brands of FDC AL medicines, comprising eight tablets and six suspensions were purchased from various retail pharmacy outlets in Kumasi, Ghana. All samples were subjected to thorough visual inspection as a quick means of checking quality through meticulous observation of the packaging or dosage form. The quality parameters of the tablets were determined using uniformity of weight, hardness, friability, and disintegration tests. Suspensions were assessed based on pH and compared with the British Pharmacopeia (BP) standard. The samples were then analyzed for drug content (assay) using reverse-phase high-performance liquid chromatography (RP-HPLC). All the tablet samples conformed to BP specification limits for uniformity of weight (deviation of less than ± 5%), hardness (4.0-10 kg/mm2), friability (<1%), and disintegration time (<15 minutes). The active pharmaceutical ingredients' quantitative assay demonstrated that all the tablets met the BP specifications (90-110%). The results of the pH studies showed that out of the six brands of suspension investigated, five (83.3%) were compliant with the official specification for pH, while one (16.7%) failed the requirement. Unlike the tablet brands, drug content analysis of the six suspensions showed that two (33.3%) were substandard. The artemether and lumefantrine contents in these failed suspensions were variable (artemether: 81.31%-116.76%; lumefantrine: 80.35%-99.71%). The study results indicate that most of the tested products met the required quality standards, demonstrating satisfactory drug content and other quality specifications. The presence of substandard drugs underscores the necessity for robust pharmacovigilance and surveillance systems to eliminate counterfeit and substandard drugs from the Ghanaian market.

Preparation, characterization, and evaluation of ketoconazole-loaded pineapple cellulose green nanofiber gel

The present study involves the isolation of cellulose nanofibers from pineapple crown waste by a combined alkali-acid treatment method. The extracted pineapple nanofibers were characterized by Fourier-transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, nuclear magnetic resonance, high-resolution transmission electron microscopy, and dynamic light scattering. The extracted pineapple nanofibers were then incorporated in Carbopol 934P containing ketoconazole to prepare a ketoconazole-loaded pineapple nanofibrous gel. The prepared gel formulation was evaluated for viscosity, spreadability, extrudibility, pH, drug content, and texture profile analysis. The anticipated gel formulation was further evaluated by in vitro drug release (98.57 ± 0.58 %), ex vivo drug permeation, cytotoxicity, and histopathological studies. The permeation of the drug through skin determined by the ex-vivo diffusion study was found to be 38.27 % with a flux rate of 4.06 ± 0.26 μg/cm2/h. Further, the cytotoxicity study of pineapple nanofiber and ketoconazole-loaded nanofiber gel displayed no cytotoxic on healthy vero cells in the concentration range from 10 to 80 μg/ml. The histopathological analysis exhibited no signs of distress and inflammation. In conclusion, ketoconazole-loaded pineapple nanofiber gel could be considered as a promising delivery system for topical applications.

Printing a cure: A tailored solution for localized drug delivery in liver cancer treatment

Adjuvant chemotherapy is highly recommended for liver cancer to enhance survival rates due to its tendency to recur frequently. Localized drug-eluting implants have gained traction as an alternative to overcome the limitations of systemic chemotherapy. This work describes the development of biodegradable 3D printed (3DP) bilayer films loaded with 5-fluorouracil (5FU) and cisplatin (Cis) with different infill percentages where the 5FU layers were 40%, 30%, and 30% and Cis layers were 10%, 15%, and 10% for films A, B, and C, respectively. The relevant characterization tests were performed, and the drug content of films was 0.68, 0.50, and 0.50 mg of 5FU and 0.39, 0.80, and 0.34 mg of Cis for films A, B, and C, respectively. Cis release was affected by the alterations to the film design, where films A, B, and C showed complete release at 12, 14, and 23 days, respectively. However, 5FU was released over 24 h for all films. The films were stable for up to two weeks after storage at 25 °C/65% relative humidity and four weeks at 4 °C where drug content, tensile strength, FTIR, and thermal analysis results demonstrated negligible alterations. The cytotoxicity of the films was assessed by MTS assays using HepG2 cell lines demonstrating up to 81% reduction in cell viability compared to blank films. Moreover, apoptosis was confirmed by Western Blots and the determination of mitochondrial cell potential, highlighting the potential of these films as a promising approach in adjuvant chemotherapy.

In situ Gel: A Promising Ocular Drug Delivery System

The eye is a vital organ, faces challenges in drug delivery with traditional ophthalmic formulations due to the rapid loss of medications before reaching the cornea. This review explores novel drug delivery systems for ocular administration, emphasizing innovative dosage forms, i.e., in situ gels. This system aims to prolong drug contact time in the eyes, overcoming bioavailability issues associated with conventional delivery methods. The article further delves into in situ gelation approaches, highlighting pH-triggered, temperature-dependent, and ion-activated systems. It explores the use of excipients like polymers and solubilizing agents in the preparation of in-situ gels. The frequently used polymers and their applications in ocular drug delivery are detailed. Studies on the incorporation of nanoparticles in this gelling system for ocular drug delivery. Methodologies for evaluating in situ gels, including pH determination, rheological studies, drug content analysis, in vitro gelation, accelerated stability studies, and FTIR analysis, are presented. The advantages &amp; applications of in situ gels are discussed, along with its limitations. The review concludes by emphasizing the benefits of novel ocular drug delivery systems, particularly in situ ophthalmic systems, which offer controlled and sustained drug release, and the future perspective of in situ gel. These advancements hold promise for more effective therapeutic outcomes in the field of ocular drug delivery.

Anti-psoriatic evaluation of aloe emodin-loaded topical hydrogel in an imiquimod-induced human plaque-type psoriasis in BALB/c mice

Aloe emodin, an anthraquinone derivative, mainly obtained from Aloe vera, possesses an extensive spectrum of pharmacological properties, including anti-proliferative, anticancer, wound healing, analgesic, anti-inflammatory, antibacterial, and antiviral properties. The objective of the present study was to prepare aloe emodin-loaded topical hydrogel formulations for managing plaque-type psoriasis. Different proportions of carbopol 940, chitosan, and hydroxyl propyl methyl cellulose K15M (HPMC K15M) were used as gelling agents. The prepared hydrogels were characterized for pH, viscosity, rheological behavior, spreadability, extrudability, swelling index, drug content, and accelerated stability. Based on physicochemical and in vitro permeation studies, PHGL1 containing aloe emodin (1%) and carbopol 940 (1%) was selected. The acute dermal toxicity study was also conducted as per the OECD guidelines 402. The mechanism of drug release followed Korsemeyer–Peppa’s model. The optimized batch showed a pH range from 6.867 ± 0.015 to 6.91 ± 0.254, drug content 94.6% ± 0.686% w/w of the active principle when studied in triplicate for drug content analysis, the measured viscosity of the formulation was 31402.33 ± 149.0783 mPaS exhibiting a shear thinning system along with thixotropic behavior at 25°C, and sustained drug release of 78% in 8 hours. An ex vivo permeation study demonstrated that 203.73 μg/ml/cm2 drug permeated through skin in 24 hours. Application of aloe emodin-loaded topical hydrogel to psoriatic skin resulted in a reduction of epidermal thickness, scaling, and ear thickness. The key inflammatory marker tissue necrosis factor (TNF-α) also showed a significant decrease. Compared with the marketed formulation, the test formulation showed no significant difference in the percentage reduction in ear thickness. No acute dermal toxicity was observed at the initial dose of 200 mg. The outcome suggests the promising potential of aloe emodin-loaded hydrogel in improving plaque-like psoriasis without dermal toxicity. Further studies are warranted to establish its efficacy in the management of psoriasis.

Development and Evaluation of Emulgel Formulation of Diclofenac Sodium utilizing Lipidium sativum as a Gelling Agent

Emulgels have gained recognition as an effective method for delivering non-polar drugs. The primary goal of our current research is to investigate the potential of Lepidium sativum seed mucilage as a gelling agent in this context. To enhance drug penetration, we have incorporated clove oil, oleic acid, and methyl salicylate. An emulsion was formulated and subsequently integrated into the gel base. Our research encompassed a series of studies, including rheological assessments, spreading coefficient evaluations, investigations into skin irritancy, and other relevant tests. Furthermore, we conducted drug content analysis, in-vitro release and permeation studies, and stability assessments. In our in-vitro investigations, it was observed that formulation E6 exhibited the highest drug release within a span of 180 minutes. Comparative analyses were conducted, pitting formulations E4, E5, and E6 against a commercially available emulgel preparation. As a result of our findings, it is evident that an emulgel employing L. sativum mucilage can effectively function as a gelling agent in a topical drug delivery system.

Computational quality-by-design strategy to validate high-performance liquid chromatography method for the estimation of meloxicam in bulk dosage forms and milk samples.

Bovine clinical mastitis has significant repercussions for farmers across the globe. Meloxicam, a COX-2 inhibitor, attenuates mastitis symptoms and is also approved for veterinary use. An RP-HPLC (Reverse Phase-High Performance Liquid Chromatography) method development and validation is essential in the pharmaceutical industry to assess API (Active Pharmaceutical Ingredient) quantity present in the pharmaceutical dosage forms. RP-HPLC method of meloxicam was developed and optimized with the aid of QbD (Quality by Design) using Box-Behnken design (BBD). The pH of the aqueous mobile phase, acetonitrile (ACN) percentage, and column temperature were chosen as influence variables, and retention time (RT) and tailing factor (Tf) were selected as response variables. The optimum experimental conditions were selected as pH ~ 3 of the aqueous mobile phase, 65% v/v ACN, and 30˚C as column temperature. The drug was eluted at 6.02min RT with 1.18 as Tf. The method was subjected to validation for accuracy, linearity, precision, range, sensitivity, and robustness and was found to comply with ICH Q2 (R1) guidelines. The in vitro bioequivalent studies were performed in hydrochloric acid, pH ~ 1.2; acetate buffer, pH ~ 4.5; and phosphate buffer, pH ~ 6.8 for two veterinary brands of meloxicam tablets, and their release profiles were compared by mathematical models. Both the brands, brand 1 and 2 exhibited significant (Unpaired t-test, P < 0.05) differences in dissolution efficiency (DE) and mean dissolution time (MDT) except DE at pH 1.2. However, brands 1 and 2 showed similarity (f2 > 50) in terms of release of meloxicam except at pH 6.8 (f2 = 47.01). The in vitro release of meloxicam followed Peppas kinetics except for brand 2 at pH 6.8, where it followed the Higuchi model. Moreover, the recovery of meloxicam extracted with ACN in the milk sample was estimated to be 99.67 ± 0.58% significantly (Unpaired t-test, P < 0.05) higher than 90.34 ± 6.77% extracted with methanol. In conclusion, the optimized and validated RP-HPLC method of meloxicam may further be used for the analysis of drug content in pharmaceutical dosage forms in addition to biological fluids.

Effects of wet granulation process variables on the quantitative assay model of transmission Raman spectroscopy for pharmaceutical tablets

Transmission Raman spectroscopy (TRS) is a process analytical technology tool for nondestructive analysis of drug content in tablets. Although wet granulation is the most used tablet manufacturing method, most TRS studies have focused on tablets manufactured via direct compression. The effects of upstream process parameter variations, such as granulation, on the prediction performance of TRS quantitative models are unknown. We evaluated the effects of process parameter variations during granulation on the prediction performance of the TRS quantitative model. Tablets with a drug concentration of 1%w/w were used. We developed PLS calibration models for the drug concentration range of 70–130% label claims. Subsequently, we predicted the drug content of the tablets with different granulation parameters. The results of our study demonstrate that the variation in the predicted recovery due to the variation in granulation parameters was practically acceptable. The calibration model showed a good prediction performance for tablets manufactured at different granulation scales and thicknesses. Therefore, we conclude that TRS quantitative models are robust to variations in upstream processes, such as granulation and downstream variations in tableting parameters. These results suggest that TRS is a versatile non-destructive quantitative analysis method that can be applied in tablet manufacturing.

Development of fast release tablet of talinolol using fourth generation carrier of solid dispersion technique

Talinolol is a beta1-selective adreno receptor antagonist well known for its Cardio protective and antihypertensive activity. Talinolol is a beta blocker. In biopharmaceutical classification system the drugs which come under class II are characterized by more membrane permeability, less dissolution rate. Talinolol is a poor aqueous solubility drug leads to poor bioavailability. So, the aimed of this study was to develop immediate release tablet of talinolol by solid dispersions technique using poloxamer 407 as a carrier. Poloxamer 407 is a hydrophilic synthetic block copolymer widely used as a solubility enhancer. Basically there are three methods used for solid dispersion. Melting or fusion method solvent evaporation method. Melting solvent method. Solvent Evaporation Method In this method a suitable solvent is selected which can capable of solubilizing both drug and hydrophilic carrier. The solvent evaporation technique is one of the most commonly used methods to prepare polymeric nanoparticles, more specifically drug-loaded polymeric systems, for pharmaceutical formulations. The prepared solid dispersions were evaluated for production yield percent, drug content, solubility, FTIR, and DSC study analysis. The prepared formulation of Talinolol with P407 in the ratio of 1:5 gave highest dissolution rate of 75.28% at 30min.So it can be concluded that the combination of solid dispersion technology as well as using superdisintergrants an encouraging and effective technique to prepare efficient fast dissolving tablets of Talinolol.The outcome of this investigation presents poloxamer 407 solid dispersion mediated fast dissolving tablets successfully resolve problem of slow rate of dissolution of talinolol.

Metoclopramide loaded buccal films for potential treatment of migraine symptoms: in vitro and in vivo study

Objective Developing mucoadhesive buccal films loaded with metoclopramide for the treatment of migraine-associated vomiting. Methods Buccal films were prepared using the solvent casting method. Several tests were conducted, including measurement of film weight, thickness, drug content, moisture uptake, swelling index, and DSC analysis. The bioadhesion properties were also assessed. Furthermore, in vitro release profiles and in human bioavailability were studied. Results The developed films were transparent, homogeneous, and easy to remove. Film weight and thickness increased with higher drug content. The drug entrapment exceeded 90%. Film weight increased with moisture uptake, and DSC analysis indicated the absence of drug crystallinity. Bioadhesion properties and swelling index decreased with increasing drug content. In vitro release demonstrated that drug release depended on the drug-polymer ratio. The in vivo study showed significant improvements in Tmax (from 1.21 ± 0.33 to 0.50 ± 0.0) and Cmax (from 45.29 ± 14.66 to 63.27 ± 24.85) compared to conventional tablets. Conclusion The prepared mucoadhesive buccal films exhibited the desired characteristics and demonstrated enhanced drug absorption, evidenced by the significantly reduced Tmax and increased Cmax compared to conventional tablets. The results indicate the successful achievement of the study objectives in selecting and designing an effective pharmaceutical dosage form. as cm2

Quality-by-design driven analytical method (AQbD) development and validation of HPLC–UV technique to quantify rivastigmine hydrogen tartrate in lipidic nanocarriers: Forced degradation, and assessment of drug content and in vitro release studies

The main purpose of current investigation was to design and further validate a technique for the quantitative determination of rivastigmine hydrogen tartrate (RHT), a cholinesterase inhibitor in the nano formulations. With the employment of a reverse phase C18 column and a very simple mobile phase, an isocratic HPLC–UV analysis technique was developed, optimized, and validated following ICH Q2 (R1) requirements along with the inculcation ofAnalytical Quality-by-Design (AQbD) methodology. A two-level full factorial screening design was applied to filter out the variables influencing responses, followed by the application of central composite design (CCD) to further optimize the method using Design-Expert® software. Analyses were performed at room temperature with 0.9 mL. min−1 flow rate and detection wavelength of 215 nm. The optimized HPLC technique exhibited superior linearity, selectivity, and precision. The inherent stability of RHT was evaluated using the optimized method byconductingforced degradation studies. The RHT peak was clear and unaffected by matrix interference in the specimens from the forced degradation studies, drug content analysis, and in vitro release study. The assay had a limit of detection (LOD) of 14.32 ng. mL−1 and a limit of quantitation (LOQ) of 43.40 ng. mL−1. With acceptable intra- and interday precision, the methodologywas confirmedto berobust. The devised stability-indicating HPLC technique for analyzing RHT content, its stability in the nano formulations, and drug release in vitro proved to be selective, accurate, sensitive, and consistent.

Solubility Enhancement of Clozapine by Co-crystals

Cocrystallization of drug with coformers is a promising approach to alter the solid state properties of drug substances like solubility and dissolution. The objective of the present work was preparation, formulation and evaluation of the clozapine cocrystal by screening various coformers. Clozapine co-crystals were prepared using different coformers like benzoic acid, fumaric acid, sodium saccharin and sodium acetate. Cocrystals were prepared using solvent evaporation method and solvent drop grinding method. The prepared co-crystals were evaluated for saturation solubility, drug content, dissolution studies, XRD studies and DSC analysis.

Effective Topical Psoralen Herbal Hydrogel Expending Capsaicin as a Penetration Enhancer

Background: This research aims to prepare a hydrogel of psoralen and capsaicin extract for topical application using various gelling agents like Carbopol 940, HPMC, Pluronic 127, and Pectin to minimize the side effect of synthetic drugs in treating psoriasis. Natural, synthetic, and semi-synthetic polymers were utilized for the treatment of psoriasis, and provide a number of benefits, including improved skin permeability, particularly for psoralen, and improved drug stability with improved therapeutic concentration gradients across the skin. Psoriasis is a T cell-mediated autoimmune disease affecting 2-3 % worldwide. Methods: FTIR and HPLC confirm the extract identification. pH, spreadability, homogeneity, extrudability, phase separation, viscosity, drug content, and stability analysis are all tested on all prepared hydrogels. The releases of psoralen from all prepared formulations are studied in phosphate buffer pH 6.8 using dialysis membranes at 37oC. Results: The net results conclude that hydrogels made using Carbopol-940 and HPMC (A1, A3, B2, B3) are the most superior and reliable formulations in terms of physicochemical parameters and in vitro permeation studies, out of which 1% carbopol 940 formulations (A3) showed maximum %CDR of 87.96 % much higher compared to other concentration used. Fitting data of the best formulations (A1, A3, B2, B3) obtained from in vitro drug permeation studies showed the release best fitted to the Korsmeyer-Peppas model as indicated by higher R2 value. The optimum formulation (A3) has a higher R2 value, which is then compared with the marketed formulation for the release of psoralen (in vitro), showing that %CDR of the A3 formulation (87.96%) is much higher than the %CDR of the marketed formulation (79.58%), due to the impact of capsaicin which acts as a penetration enhancer and therefore increases psoralen release from the hydrogel. Conclusion: As a result, the permeability issue with Psoralen for dermal drug administration has been overcome by using capsaicin as a permeability enhancer.

Cyclodextrin-based nanogel of flurbiprofen for dermal application: In vitro studies and in vivo skin irritation evaluation

The aim of this study was to develop and characterize flurbiprofen (FB)-loaded cyclodextrin (CD) based nanogel formulations for dermal application. Nanogels were produced via emulsification solvent evaporation and then incorporated into a hydroxypropyl methyl cellulose (HPMC) gel. The visual examination, pH, viscosity, dynamic rheological measurements and drug content analysis of nanogels were assessed. In vitro and ex vivo permeation, stability, and skin irritation were performed. pH of the FB-loaded nanogel and the nanogels in HPMC were 10.6 ± 0.1 and 7.5 ± 0.1 (neutral) respectively. The highest and lowest viscosities were observed in FB-loaded nanogels and in FB-free nanogels in HPMC, respectively. The tangent δ and storage modulus values of FB-loaded nanogel in HPMC were higher than those of FB-loaded nanogel. FB from nanogels in HPMC was 100% by 48 h. The final nanogel formulation was physically and chemically stable over 12 months. Skin irritation test showed no skin irritation or cellular infiltration on the histological level. In vitro and ex vivo permeation showed that the nanogels could be effective and stable formulations, especially in the dermal application of a hydrophobic molecule.

Development of Solid Self Nanoemulsifying Drug Delivery System of Quercetin

This work aims to develop Solid Self Emulsifying Drug Delivery System of Quercetin for enhancing its bioavailability. From the perspective of dosage forms, Solid Self Emulsifying Drug Delivery System mean solid dosage forms with self-emulsification properties. Liquid Self Emulsifying Drug Delivery System containing 15 mg/ml of Quercetin was prepared and converted to Solid Self Emulsifying Drug Delivery System by adsorption onto various solid carriers. Based on micromeritic properties and drug content analysis Aerosil ® 200 was selected as the adsorbent for development of Solid Self Emulsifying Drug Delivery System of Quercetin.Various formulation were prepared by variying amounts of the components and optimized fornulation showed particle size of 264.2 nm and drug content of 93.95 %.Optimized Solid Self Emulsifying Drug Delivery System of Quercetin showed good self emulsification ,absence of interactions(FTIR analyis), solubilization of the drug in the mixture (DSC and XRD analysis)and smooth surface (SEM analysis ) . In-vitro drug release of Solid Self Emulsifying Drug Delivery System of Quercetin revealed percentage drug release of 99.70±0.227% within 30 min . Results of the study indicates the Solid Self emulsification technique is a promising approach for development of stable dosage form of drugs with poor oral absorption.

Formulation of mucoadhesive mouth paint for oral infections

Oral mucoadhesive mouth paint preparation was designed and prepared for the treatment of oral candidiasis, where prolonged drug release at the infected area is essential. Fluconazole, a recent triazole derivative having antifungal activity is chosen as the desired drug in this study to formulate mucoadhesive mouth paint. Oral candidiasis is a common infection in debilated patients, AIDS patients and in persons who administer immunosuppressive drugs. Mouth paints containing 1% fluconazole with hydrophilic polymer HPMC was prepared and compared with mouth paint prepared without the addition of hydrophilic polymer. The prepared mouth paint formulation was subjected to various evaluation parameters like pH determination, drug content, rheological behavior, mucoadhesive studies, spreadability and IR spectral analysis. In vitro drug release studies were carried out at salivary pH 6.4 using cellophane membrane as barrier. Stability studies were carried out at different temperature conditions like ambient temp (R. T.), 8 ± 1oC, 45 ± 2oC at 75% ± 5% R. H. (accelerated temperature) 3 months and analyzed at different time intervals for drug content, physical appearance, pH, mucoadhesive strength and spreadability and the prepared formulation was found to be stable. Antimicrobial studies were carried out to ascertain the antifungal activity of prepared mucoadhesive formulation against the pure drug. The test organism Candida albicans was a clinical isolate obtained from a diseased patient suffering from oral Candidiasis. In vitro antifungal activity was evaluated using standard Agar cup-plate method by zone inhibitions studies. Formulations, containing HPMC showed good zone inhibition. In vivo oral mucosal skin irritancy tests were carried out using mucoadhesive formulation on lab experimental animals (Rabbits and Guinea-pigs) and on healthy human volunteers. No edema, erythema, inflammation or redness in the mucosal cavity of both animals and human volunteers were observed.