Mucoadhesive Formulation Research Articles

MACROSCOPIC AND MICROSCOPIC GASTROPROTECTIVE ACTIVITY OF MUCOADHESIVE GRANULE FORMULATIONS OF CLOVE LEAF ETHANOL EXTRACT

Gastric ulcers can be triggered by excessive HCl secretion, and the regenerative capacity of mucosal cells can be weakened by high alcohol levels and anti-inflammatory drugs, including NSAIDs. This study aims to evaluate the macroscopic and microscopic gastroprotective activity of clove leaf ethanol extract mucoadhesive granule formulations. The study used 25 rats divided into five groups: normal control, negative control, positive control, clove leaf ethanol extract group, and mucoadhesive granule formulation of clove leaf ethanol extract group. All groups except the normal control were administered acetylsalicylic acid. Treatments were conducted over 9 days, with surgical examination and observations performed macroscopically and microscopically on day 10. Macroscopic assessments revealed ulcer damage improvement in the positive control, extract, and mucoadhesive granule groups, all scored at 1. Microscopic assessments also indicated a significant difference between the negative control and the positive control, extract, and mucoadhesive granule groups, showing better gastric repair, scored at 0.5. Therefore, it can be concluded that the administration of the mucoadhesive granule formulation of clove leaf ethanol extract exhibits gastroprotective activity comparable to that of the clove leaf ethanol extract

Acute Toxicity Test of Gastroretentive Mucoadhesive Granule Preparation of Earthworm Flour (Lumbricus rubellus)

Earthworms (Lumbricus rubellus) contain the compound lumbricin, which is beneficial for treatment, and its use is still simple, leading to the innovation of gastroretentive mucoadhesive granule formulations. However, its security has not yet been fully supported by research. This research aims to determine the toxic effects caused by earthworm granule preparations in terms of toxicity symptoms and the determination of the LD50 value. This research used 20 male white rats that were randomly divided into 4 groups. One control group was given Aquadest, and three treatment groups were given earthworm granules at doses of 500 mg/kgBB (P1), 2000 mg/kgBB (P2), and 5000 mg/kgBB (P3) with a single oral administration. The research results indicate that the preparation of earthworm granules (Lumbricus rubellus) causes toxic symptoms such as decreased locomotor activity, piloerection, and increased grooming frequency in line with the increase in dosage, but does not result in the death of the test animals. (LD50). Based on the research findings, it can be concluded that the LD50 value of the earthworm granules (Lumbricus rubellus) is >5000 mg/kgBB and falls into the practically non-toxic category with an LD50 range of 5–15 g/kgBB

Mucoadhesive and drug release of cholic acid based thiomeric micelles and encapsulated silver and gold nanoparticles for anticancer studies

Among the various drug delivery system, mucoadhesive formulation is a promising approach to deliver drugs and vaccine through close contact with the absorption site and mucous membrane. Bile acids have received considerable interest in drug delivery (DD) applications owing to their advantages of biocompatibility, ability to act as both drug solubilizing and permeation-modifying agents. In this aspects, cholic acid (CA) based thiomeric micelles with improved mucoadhesive properties have been synthesized by functionalization of thiol groups and conjugation of PEG. The synthesized CA based thiomeric micelles (TCA-PEG) were characterized by 1HNMR, ATR-IR, GPC, Zeta potential and contact angle techniques. The critical micelle concentration (CMC) of TCA-PEG was measured by a fluorescence spectrometer using pyrene as a probe. The mucoadhesive properties of TCA-PEG polymeric micelles (PMs) were examined on the goat anterior tongue mucosa with an effectively higher adhesion of 40 % up to 3 h study period. Also, curcumin loaded TCA-PEG PMs showed only 13 % of the drug released up to the period of 3 h. The TCA-PEG PMs act as reducing and stabilizing agents for the preparation of gold and silver nanoparticle (Ag and Au NPs) and were characterized by UV–visible, DLS, Zeta potential, XPS, and HR-TEM techniques. The cytotoxicity and cellular apoptosis of TCA-PEG PMs encapsulated Ag and Au NPs were examined by MTT assay and AO/PI dual staining using MCF-7 breast cancer cells wherein AgNPs showed an effective cytotoxicity than AuNPs. The developed TCA-PEG PMs act as reservoir for soubilization of hydrophobic and hydrophilic drugs and ideal template for encapsulation of silver and gold nanoparticles for mucoadhesive DD system.

Design of experiment (DoE) of mucoadhesive valproic acid-loaded nanostructured lipid carriers (NLC) for potential nose-to-brain application

Epilepsy is a highly prevalent neurological disease and valproic acid (VPA) is used as a first-line chronic treatment. However, this drug has poor oral bioavailability, which requires the administration of high doses, resulting in adverse effects. Alternative routes of VPA administration have therefore been investigated, such as the nose-to-brain route, which allows the drug to be transported directly from the nasal cavity to the brain. Here, the use of nanostructured lipid carriers (NLC) to encapsulate drugs administered in the nasal cavity has proved advantageous. The aim of this work was to optimise a mucoadhesive formulation of VPA-loaded NLC for intranasal administration to improve the treatment of epilepsy. The Design of Experiment (DoE) was used to optimise the formulation, starting with component optimisation using Mixture Design (MD), followed by optimisation of the manufacturing process parameters using Central Composite Design (CCD).The optimised VPA-loaded NLC had a particle size of 76.1 ± 2.8 nm, a polydispersity index of 0.190 ± 0.027, a zeta potential of 28.1 ± 2.0 mV and an encapsulation efficiency of 85.4 ± 0.8%. The in vitro release study showed VPA release from the NLC of 50 % after 6 h and 100 % after 24 h. The in vitro biocompatibility experiments in various cell lines have shown that the optimised VPA-loaded NLC formulation is safe up to 75 µg/mL, in neuronal (SH-SY5Y), nasal (RPMI 2650) and hepatic (HepG2) cells. Finally, the interaction of the optimised VPA-loaded NLC formulation with nasal mucus was investigated and mucoadhesive properties were observed. The results of this study suggest that the use of intranasal VPA-loaded NLC may be a promising alternative to promote VPA targeting to the brain, thereby improving bioavailability and minimising adverse effects.

DoE-Aided Optimization of RP-HPLC Method for Simultaneous Estimation of Amoxicillin and Tinidazole Loaded Mucoadhesive GRDDS Formulation for the Treatment of H. pylori

Helicobacter pylori (H. pylori) infection is one of the primary risk factors of peptic ulcer disease worldwide. Treatment of H. pylori with the conventional dosage form is often challenging due to the ineffective reach of the antibiotics to the inner layers of gastric mucosa, where the organism resides. This study developed an eco-friendly, stability-indicating RP-HPLC method to simultaneously estimate amoxicillin and tinidazole from mucoadhesive formulation targeting H. pylori infection. The mucoadhesive GRDDS formulation of antibiotics was developed with a goal of improving bioavailability at the gastric mucosa. The multivariate Box–Behnken design (BBD) was utilized to optimize chromatographic parameters. Independent variable such as ratio of mobile phase, flow rate, pH and injections volume were optimized using DoE, and analyzed using perturbation plots. A desirability of 0.981 was achieved for the optimized variables. The optimized method utilized methanol and phosphate buffer (25:75) at pH 6.3 as the mobile phase in an isocratic elution mode on a Luna ODS C18 column kept at 25 °C as the stationary phase. The method was linear from 0.25 to 20 µg/mL, for both the drugs with R2 values of 0.9993 and 0.9997 for amoxicillin and tinidazole, respectively. This validated RP-HPLC technique demonstrated selectivity in the presence of possible degradation products and excipients present in the mucoadhesive GRDDS beads. The method was used for the determination of entrapment efficiency and in vitro release profile for tinidazole and amoxicillin in the mucoadhesive GRDDS formulation.Graphical

Chitosan-coated liposomal systems for delivery of antibacterial peptide LL17-32 to Porphyromonas gingivalis

Periodontal disease is triggered by surface bacterial biofilms where bacteria are less susceptible to antibiotic treatment. The development of liposome-based delivery mechanisms for the therapeutic use of antimicrobial peptides is an attractive alternative in this regard. The cationic antimicrobial peptide LL-37 (human cathelicidin) is well-known to exert antibacterial activity against Porphyromonasgingivalis, a keystone oral pathogen. However, the antibacterial activity of the 16-amino acid fragment (LL17-32) of LL-37, is unknown. In addition, there are still gaps in studies using liposomal formulations as delivery vehicles of antibacterial peptides against this pathogen. This study was designed to examine the influence of the different types of liposomal formulations to associate and deliver LL17-32 to act against P. gingivalis. Chitosans of varying Mw and degree of acetylation (DA) were adsorbed at the surface of soya lecithin (SL) liposomes. Their bulk (average hydrodynamic size, ζ-potential and membrane fluidity) and ultrastructural (d-spacing, half-bilayer thickness and the water layer thickness) biophysical properties were investigated by a panel of techniques (DLS, SAXS, M3-PALS, fluorescence spectroscopy and TEM imaging). Their association efficiency, in vitro release, stability, and efficacy in killing the periodontal pathogen P. gingivalis were also investigated. All liposomal systems possessed spherical morphologies and good shelf-life stabilities. Under physiological conditions, chitosan formulations with a high DA demonstrated enhanced stability in comparison to low DA-chitosan formulations. Chitosans and LL17-32 both decreased SL-liposomal membrane fluidity. LL17-32 exhibited a high degree of association with SL-liposomes without in vitro release. In biological studies, free LL17-32 or chitosans alone, demonstrated microbicidal activity against P. gingivalis, however this was attenuated when LL17-32 was loaded onto the SL-liposome delivery system, presumably due to the restrained release of the peptide. A property that could be harnessed in future studies (e.g., oral mucoadhesive slow-release formulations).

Muco-Adhesive and Muco-Penetrative Formulations for the Oral Delivery of Insulin.

Insulin, a pivotal anabolic hormone, regulates glucose homeostasis by facilitating the conversion of blood glucose to energy or storage. Dysfunction in insulin activity, often associated with pancreatic β cells impairment, leads to hyperglycemia, a hallmark of diabetes. Type 1 diabetes (T1D) results from autoimmune destruction of β cells, while type 2 diabetes (T2D) stems from genetic, environmental, and lifestyle factors causing β cell dysfunction and insulin resistance. Currently, insulin therapy is used for most of the cases of T1D, while it is used only in a few persistent cases of T2D, often supplemented with dietary and lifestyle changes. The key challenge in oral insulin delivery lies in overcoming gastrointestinal (GI) barriers, including enzymatic degradation, low permeability, food interactions, low bioavailability, and long-term safety concerns. The muco-adhesive (MA) and muco-penetrative (MP) formulations aim to enhance oral insulin delivery by addressing these challenges. The mucus layer, a hydrogel matrix covering epithelial cells in the GI tract, poses significant barriers to oral insulin absorption. Its structure, composition, and turnover rate influence interactions with insulin and other drug carriers. Some of the few factors that influence mucoadhesion and mucopenetration are particle size, surface charge distribution, and surface modifications. This review discusses the challenges associated with oral insulin delivery, explores the properties of mucus, and evaluates the strategies for achieving excellent MA and MP formulations, focusing on nanotechnology-based approaches. The development of effective oral insulin formulations holds the potential to revolutionize diabetes management, providing patients with a more convenient and patient-friendly alternative to traditional insulin administration methods.

Chitosan-based buccal mucoadhesive bilayer tablets enhance the bioavailability of tizanidine hydrochloride by bypassing the first-pass metabolism

Tizanidine hydrochloride (TZN) is an antimuscarinic agent used in the treatment of pain-related spasms, multiple sclerosis, and stroke-related spasticity. It has low oral bioavailability (40 %) due to excessive first-pass metabolism in the liver. The aim of this project was to enhance the systemic bioavailability of TZN by developing buccal mucoadhesive bilayer tablet formulations using chitosan salts with molecular weights of 136 kDa (7 cP) and 169 kDa (10 cP). Structural characterisation of chitosans and their salts was performed by FTIR, 1H NMR, DSC, TGA, and XRD analyses. Soluble chitosan salts, chitosan glutamate and chitosan chloride, for the adhesive layer, and insoluble ethyl cellulose for the impermeable backing layer were selected as polymers to fabricate the buccal tablets by direct compression method. The tablets containing TZN demonstrated high swelling and good mucoadhesion characteristics as well as released all the drug within 8 h. While TC10, formulated with 10 cP chitosan chloride, showed the highest swelling properties, TG10, prepared with 10 cP chitosan glutamate, exhibited the highest mucoadhesion. Chitosan glutamate tablets (TG7 and TG10) demonstrated better mucoadhesive characteristics and stability than chitosan chloride ones (TC7 and TC10) in the buccal medium based on the results of swelling and drug release studies. The permeability studies performed by Franz diffusion cell demonstrated that the amount of TZN passing through the bovine buccal mucosa was between 13.4 and 14.4 %. Stability studies conducted at 5 ± 2 °C, 25 ± 2 °C and 40 ± 2 °C for 6 months showed that no changes in the content uniformity and pH were observed. The in vivo comparative bioavailability studies in female New Zealand rabbits were performed and TZN-containing buccal mucoadhesive bilayer tablets fabricated with both chloride (TC10) and glutamate (TG10) salts of chitosan demonstrated three times higher bioavailability than the commercial TZN product (Sirdalud® oral tablet) administered by the gastrointestinal route.

Mucoadhesion, Rheology, Swelling Behavior, and Immunomodulatory Properties of Polysaccharides of Gum Exudates Obtained from Astracantha echidnaeformis (Sirj.) Podlech as a Formulary Excipient Candidate

AbstractThe physicochemical, rheological, and mucoadhesive characteristics of gum derived from Astracantha echidnaeformis are investigated. It's polysaccharides are isolated using chromatography techniques, and their immunomodulatory characteristics are evaluated by subjecting Jurkat cells to the WST‐1 assay. The composition of these polysaccharides is analyzed using gas chromatography‐mass spectrometry (GC‐MS). The viscosity and shear‐thinning behavior of gum are directly influenced by its concentration and the presence of NaCl, whereas they are inversely affected by temperature. The gum has strong potential as a thickening agent for dispersed systems. The mucoadhesion strength of the gum insoluble fraction is 109 ± 4.58 g cm−2, indicating excellent adhesiveness for application to mucoadhesive formulations. Cells’ proliferation enhancement is found for the isolated manno‐arabinoglucan (MW: ≤1.27 kDa) and galacto‐arabinan (MW: ≥667.8 kDa) at concentrations lower than 400 µ mL−1, but at higher concentrations they inhibited the proliferation. The isolated pectic galacto‐arabinan (MW: 669.58 kDa) exhibited a proliferative effect at 250 µg mL−1, but the isolated manno‐galactoglucan (MW: 80.90 kDa) showed cytotoxicity at higher doses. The isolated proteoglycans has mostly galacto‐arabinan backbones with immunomodulatory properties. The gum can be used as a thickening agent for the physical stabilization of suspensions and gels, specifically those needing to be stored at cold temperatures.

Development of mucoadhesive microspheres for intranasal delivery of fluconazole as an alternative treatment of cryptococcal meningitis infection in patients with acquired immunodeficiency

Cryptococcal meningitis is a deadly disease with few treatment options. Its incidence is still high and closely linked to the HIV/AIDS epidemic. This study aimed to develop a mucoadhesive microsphere delivery system for fluconazole for the intranasal route. Microspheres of mucoadhesive fluconazole formulation variables such as different amounts of drug concentration and polymer concentration were prepared by a simple emulsion-crosslinking method.The prepared microspheres' surface was characterised by SEM (Scanning electron microscopy) and evaluated for particle size, entrapment efficiency, production yield, infrared spectroscopic study, in-vitro muco-adhesion, and in-vitro drug release. The results showed that formula 1 is the optimal mucoadhesive microsphere preparation, with a particle size of 56.375m, a spherical surface shape, an entrapment efficiency of 99.96%, and a greater mucoadhesive capability during 6-hour evaluation. Furthermore, wash-off examination revealed that the mucoadhesive ability of this delivery system has a long duration and may release the active material at the right time. The result of the researches suggesting that the formulation of mucoadhesive microspheres of fluconazole could be used to treat cryptococcal meningitis infection in HIV/AIDS patients.

Formulation and Evaluation of Natural Excipient-based Mucoadhesive Salbutamol Sulphate Tablets

When creating a mucoadhesive sustained-release formulation for oral consumption, aquaphilic matrices are a captivating option to consider. These aquaphilic matrices are used to release water-soluble and water-insoluble drugs. Gums and mucilages used in the current study are linseed mucilage (LM) and tamarind seed polysaccharide (TSP). The present work aims to focus on the possibilities of using these polysaccharides to prepare a new medication delivery system. The aim of the research was to make a salbutamol sulfate mucoadhesive tablet for the treatment of asthma. The wet granulation method was adopted for the formulation of the salbutamol sulfate mucosal adhesive tablet. Mucosal adhesive tablets were assessed for multiple parameters. The drug release is low as the amount of gums and mucilages is high. A mucoadhesive tablet containing linseed mucilage and chitosan exhibits good mucoadhesive performance and in-vitro drug release. Optimized formulation FM1 fits the Higuchi plot of release kinetics

Unlocking traditional remedy: Gulkand-enhanced mucoadhesive gel for canker sore relief

This study focuses on the development and evaluation of mucoadhesive gel formulations containing different Gulkand and its extract with a specific emphasis on their potential for managing oral health conditions, including the discomforting issue of mouth ulcers. The formulations underwent a thorough analysis, encompassing the assessment of phenolic compounds responsible for antioxidant activity, in addition to comprehensive physical, chemical, and pharmacological evaluations to determine their suitability for commercial utilization. Mouth ulcers are a prevalent oral health concern that can cause significant discomfort and inconvenience. In this study, Gulkand extract exhibited remarkable characteristics with its high phenolic content and robust antioxidant activity. It demonstrated rapid drug release, positioning it as a promising new for addressing the immediate relief needs of individuals suffering from mouth ulcers. Conversely, gel formulation showcased a sustained release profile suggesting the potential for longer therapeutic benefits, presents an intriguing option for oral health applications, capitalizing on the antiulcer properties associated with liquorice. An innovative aspect of this study is the compatibility assessment, which employed antioxidant and phenolic content analysis to verify the harmonious interaction between herbal constituents and excipients. This approach introduces novel perspective on compatibility testing, particularly critical for formulations designed to alleviate oral discomfort effectively. Furthermore, stability studies are warranted to be evaluated prior to their potential for commercialization. The present study revealed the promising potential of the prepared mucoadhesive gels in managing not only mouth ulcers but also a spectrum of oral health conditions, holding broader implications for advancements in the field of medicine.

Clinical pharmacokinetics of atropine oral gel formulation in healthy volunteers.

Sialorrhea or drooling is a common problem in children and adults with neurodevelopmental disorders. It can negatively impact the quality of life due to its physical and psychological manifestations. Providers commonly prescribe atropine eye drops for topical administration to the oral mucosa, as an off-label treatment to manage sialorrhea. However, the off-label use of atropine eye drops can be associated with medication and dosing errors and systemic side effects. To address these limitations of treatment, we developed a mucoadhesive topical oral gel formulation of atropine as an alternative route to off-label administration of atropine eye drops. In this clinical pharmacokinetic (PK) study, we evaluated the safety and PK of atropine gel (0.01% w/w) formulation after single-dose administration to the oral mucosa in 10 healthy volunteers. The PK data showed that after topical administration to the oral mucosa, atropine followed a two-compartment PK profile. The maximum plasma concentration and area under the curve extrapolated to infinite time were 0.14 ng/mL and 0.74 h·ng·mL-1 , respectively. The absorption rate constant calculated by the compartmental analysis was 0.4 h-1 . Safety parameters, such as heart rate, blood pressure, and oxygen saturation, did not significantly change before and after administration of the gel formulation, and no adverse events were observed in all participants who received atropine gel. These data indicate that atropine gel formulation has a satisfactory PK profile, is well-tolerated at the dose studied, and can be further considered for clinical development as a drug product to treat sialorrhea.

Quality by Design Enabled Formulation Optimization of Rabeprazole Sodium Mucoadhesive Microcapsules for the Treatment of Gastroesophageal Reflux Disease

Aims: The present research describes the implementation of quality by-design principles for developing the mucoadhesive microcapsules of rabeprazole sodium for treating gastroesophageal reflux disease conditions. Background: In addition, a holistic QbD-based product development strategy was implemented, where the target product profile was defined based on desired product quality of mucoadhesive microcapsules. Based on TPP, the critical quality attributes were identified. The identification of CMAs was carried out with the help of risk assessment and factor screening exercises, which indicated drugpolymer ratio (X1), temperature (X2), and stirring speed (X3) as the influential factors. Methods: The mucoadhesive microcapsules of rabeprazole sodium were prepared by a solvent evaporation method, and 33 Box-Behnken optimization design was used for the optimization of the selected factors, and mucoadhesive microcapsules formulations were evaluated for particle size (μm), drug entrapment efficiency (%), mucoadhesion (%), and in vitro drug release (Q18h) in percentage characteristics. Mathematical data analysis was performed to fit the two-factor interaction model, and optimized mucoadhesive microcapsules formulation was selected. Results: The optimized mucoadhesive microcapsules indicated desired formulation characteristics with smaller particle size, good entrapment efficiency, better mucoadhesion, and sustained drug release characteristics. Conclusion: In a nutshell, the studies vouch for the successful development of mucoadhesive microcapsules for oral delivery of rabeprazole sodium which could be used to manage gastroesophageal reflux disease condition.

Spray-Dried Mucoadhesive Re-dispersible Gargle of Chlorhexidine for Improved Response Against Throat Infection: Formulation Development, In Vitro and In Vivo Evaluation.

Drug delivery to the buccal mucosa is one of the most convenient ways to treat common mouth problems. Here, we propose a spray-dried re-dispersible mucoadhesive controlled release gargle formulation to improve the efficacy of chlorhexidine. The present investigation portrays an approach to get stable and free-flowing spray-dried porous aggregates of chlorhexidine-loaded sodium alginate nanoparticles. The ionic gelation technique aided with the chlorhexidine's positive surface charge-based crosslinking, followed by spray drying of the nanoparticle's dispersion in the presence of lactose- and leucine-yielded nano-aggregates with good flow properties and with a size range of about 120-350nm. Provided with the high entrapment efficiency (87%), the particles showed sustained drug release behaviors over a duration of 10h, where 87% of the released drug got permeated within 12h. The antimicrobial activity of the prepared formulation was tested on S. aureus, provided with a higher zone of growth inhibition than the marketed formulation. Aided with an appropriate mucoadhesive strength, this product exhibited extended retention of nanoparticles in the throat region, as shown by in vivo imaging results. In conclusion, the technology, provided with high drug retention and extended effect, could be a potential candidate for treating several types of throat infections.

Development of an efficient biocomposite hydrogel with enhanced mucoadhesive and antibacterial properties

Noteworthy, mucoadhesion is considered an effective approach in drug delivery. Indeed, mucoadhesion donates various advantages including prolonged residence time, drug preservation, enhanced drug permeation, and developed drug accessibility. Herein, a novel gelatin based mucoadhesive hydrogel noted as gelatin/EudragitL100/Xanthan gum in combination with TiO2 and CuO metal oxides were fabricated with the aid of a facile preparation approach. In fact, the main goal of this research study is to utilize this formulation as a mucoadhesive hydrogel for the treatment of aphthous ulcers cases. To achieving and address the appropriate mucoadhesive formulation, the effect of plasticizers (PEG4000 and PG) and surfactant (SLS), kind of metal oxide and weight percent of biopolymer in formulation was studied in details. It is significant that a semi-solid formulation was obtained and examined in all experiments. Based on the results, the existence of xanthan gum, CuO and TiO2 in conjunction with Gelatin/EudragitL100 enhances the efficiency of the mucoadhesive hydrogel. It is significant that a semi-solid formulation was obtained and examined in all experiments. The as-prepared hydrogel (M7) was characterized by Fourier transform infrared (FTIR) and scanning electron microscopy (SEM). The ex vivo mucoadhesive investigation displays that the designed hydrogel possesses a convenient adhesive and biodegradation feature. The gelatin/EudragitL100/Xanthan gum/TiO2/CuO hydrogel exposed biocompatibility > 70 % for MTT assay. The in vitro swelling ratio has diminished at basic pH, owing to the smaller pore sizes, which diminishes the water absorption. Antibacterial characteristics of hydrogel (Gelatin/EudragitL100/ Xanthan gum /TiO2/CuO) on various bacteria including Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Lactobacillus plantarum and Streptococcus mutans was evaluated. The fungal surveyed species was Candida albicans ATCC 10231. The highest and lowest inhibitory effects were reported on Candida albicans and Lactobacillus plantarum, respectively. DPPH results illustrated that M7 has an appropriate radical scavenging property compared to that of reference models. All in all, the present research study addresses a significant perception regarding the utilization of mucoadhesive formulation for practical applications.

Rasagiline mesylate mucoadhesive buccal microsphere-loaded gel formulations: a new candidate for non-oral parkinson"s treatment

Rasagiline mesylate mucoadhesive buccal microsphere-loaded gel formulations: a new candidate for non-oral parkinson"s treatment

Box-Behnken guided development of an ecofriendly RP-HPLC analytical method for simultaneous quantification of pantoprazole sodium and piperine co-loaded mucoadhesive GRDDS formulation for H. pylori eradication

Helicobacter pylori (H. pylori) infection is the leading cause of chronic peptic ulcer disease worldwide. Many treatment options are available to treat H. pylori infection. However, the eradication is still a challenge due to the poor bioavailability of the currently available formulations. To improve the efficacy of therapy, novel formulations are necessary. Proton pump inhibitors (PPIs) are already a part of the treatment regimen with antibiotics. P-glycoprotein (P-gp) inhibitor was reported to have increased the efficacy of antibiotic treatment in H. pylori infections. To make available the P-gp inhibitor and PPI on the intestinal mucosal surface we have formulated a gastroretentive drug delivery system (GRDDS) as an adjuvant therapy with antibiotics. The objective of this study is to simultaneously estimate pantoprazole (PAN) and piperine (PIP) by reverse-phase (RP) high-performance liquid chromatography (HPLC) method from the chitosan-based sodium alginate mucoadhesive beads utilizing the design of experiments (DOEs) methodology. The HPLC settings were optimized using DOEs software. The final optimized HPLC method used a hyperclone Octadecylsilane C18 column as the stationary phase and methanol: ammonium acetate at pH 4.5 (70:30 v/v) as the mobile phase. The flow rate was 0.9 ml/minute. The validation of the developed RP-HPLC method was done as per the International Conference on Harmonization (ICH) Q2(R1) guideline. The method was linear from 0.5 to 20 μg/ml for both PAN and PIP with an R2 value of 0.999 and 0.999, respectively. The validated RP-HPLC method showed specificity for both drugs despite interference from degradation products and other GRDDS excipients. The entrapment efficiency of the final formulation was determined to be 80%–85% for PAN and 60%–67% for PIP. The novelty and merit of the DOE-based method development are that it reduces the number of trials, thereby reducing reagent wastage, and is environmentally friendly suggested by the Green Analytical Procedure Index (GAPI) tool scoring six green, six yellow, and three red.

Frovatriptan succinate intranasal delivery for brain targeting – in vivo study.‎

Muco-adhesive gel formulations are advantageous in extending the stay at the nasal ‎absorption place, promoting drug absorption. Frovatriptan succinate (FVT) exhibits a 35% ‎oral bioavailability and undergoes hepatic metabolism, making it a viable candidate for ‎nasal delivery. This study aimed to assess novel FVT intranasal formulation for brain ‎targeting in rat animal models. A total of 78 female rats (Rattus norvegicus domestica, ‎Wister albino rats) were randomly divided into three groups: group A (considered a ‎negative control), group B (includes 36 rats given FVT IV solution), and group C (includes ‎‎36 rats given FVT binary ethosome in situ gel intranasally). Drug levels in plasma and brain ‎tissue were measured using HPLC methods. In all periods, for both brain tissue ‎concentrations of FVT and the brain-to-plasma ratio of FVT, it was significantly higher in ‎Group C compared to Group B. Nasal administration of FVT showed higher brain Tmax, ‎Cmac, and AUC compared to IV administration, with 239.83% higher accumulation of FVT ‎when nasal formulation used compared to IV administration. In conclusion, in situ gel has ‎demonstrated its efficacy in facilitating the delivery of frovatriptan succinate via the nasal ‎route. The convenience of the administration process, combined with reduced frequency of ‎administration, contributes to improved patient adherence‎‎‎.

DoE Guided Development of an HPLC Method for Evaluation of Amoxicillin and Metronidazole Co-loaded Mucoadhesive GRDDS Formulation for H. pylori Eradication

DoE Guided Development of an HPLC Method for Evaluation of Amoxicillin and Metronidazole Co-loaded Mucoadhesive GRDDS Formulation for H. pylori Eradication