Excipient Compatibility Research Articles

Formulation Design and In-vitro Characterization of Docetaxel Cubosomes for Gastric Cancer therapy

Cubosomes are altered cubic phase systems, which are emerging as promising drug delivery system for the delivery of both hydrophilic and lipophilic drugs. Docetaxel is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumors including breast and lung cancer. Docetaxel in the form of cubosomes. The main aim of present research was to encapsulate, Docetaxel in cubosomes for sustained drug release. Docetaxel loaded cubosomes were prepared by Bottom-Up Method technique using Glyceryl Mono Oleate and pluronic F-127 and Pluronic F68 in different ratios. The prepared formulations were subjected to evaluation studies for excipient compatibility, particle size, drug content, entrapment efficiency and In vitro drug release. The maximum entrapment efficiency was found as 90.15% with, and In vitro drug release as 99.37%. Stability studies were also conducted for the formulations as per protocol mentioned in ICH guidelines. These results suggest that the cubosomal formulation F4 is suitable for the delivery of Docetaxel.

Tenofovir Alafenamide Fumarate Microspheres, Process Parameters for Enhanced Permeability and Liver Targeting

Aims: Chronic hepatitis B (CHB) infection is a serious global health problem and one of the main causes of chronic liver disease, cirrhosis. Tenofovir Alafenamide Fumarate (TAF) is a prodrug of Tenofovir, a nucleotide analogue with limited oral bioavailability. TAF is considered to be a BCS Class III substance (high solubility, low permeability). The aim of the study was to develop the Tenofovir Alafenamide Fumarate (TAF) microspheres to improve permeability.
 Study design: Preparation and Evaluation of Microspheres.
 Place and Duration of Study: Department of pharmaceutics, Mallareddy Institute of Pharmaceutical Sciences, Affiliated to JNTUH, Hyderabad, Telangana, India, between January 2018 and June 2019.
 Methodology: TAF loaded chitosan microspheres were prepared by emulsion cross linking method using glutaraldehyde as cross-linking agent. The prepared microspheres were characterized by morphology, size distribution, encapsulation efficiency. The permeability study was evaluated by Ex-vivo permeation studies. The optimized formulation was subjected to FTIR studies to examine the Drug Excipient Compatibility.
 Results: Scanning Electron Microscopy (SEM) studies indicated that the microspheres are spherical in shape. The optimized formulation has average particle size of 11.00 ± 0.05 µm, the encapsulation efficiency 68
 ± 0.04% and the percentage (%) yield of 94%. FTIR studies indicated that the drug and polymer are compatable with each other. In Ex-vivo permeation studies of optimized formulation 80% of drug was permeated with in 60 min.
 Conclusion: TAF microspheres could improve the absorption by increasing the permeability.

Development of gastroretentiv floating tablets of losartan potassium by sublimation method

The purpose of present study was to formulate and Evaluate Sustained release floating tablet of losartan Potassium using Camphor and Polyethylene Oxide as Pore formation for floating and release retarding agent respectively to improve gastric residence time and patient compliance in management of hypertension. The tablet was prepared by direct compression by using HPMC K4 as dry binder. Camphor and PEO as floating and release retarding agent for sustained release floating tablet. Post compression was done to increase the hardness and floating time of tablet. Release modifier was used to speed up the release of drug from sustained release floating tablet. The effect of two independent variables like amount of Sublimating agent (camphor) and amount of Polyethylene oxide (PEO) on Q30min, Q360min, and Q720min was optimized using 32 factorial design and analyzed using the software design expert 10.0.3. The observed (actual values) responses were coincided well with the predicted values, given by the optimization technique. The floating tablet were characterized by FTIR for drug excipient compatibility.

Formulation and Invitro evaluation of immediate release tablets containing febuxostat

In the present research work, Febuxostat Immediate Release Tablet was prepared by direct compression method using varying concentrations of Lycoat, Crospovidone& Croscarmellose sodium as disintegrants. The formulations prepared were evaluated for precompression& post-compression parameters. From the drug excipient compatibility studies, we observe that there are no interactions between the pure drug (Febuxostat) and optimized formulation (Febuxostat+ excipients) which indicates there are no physical changes. Post compression parameters were found to be within the limits. Among the formulation prepared the tablet containing 12mg of CCS shows 98.13% of the drug release within 45 min & follows first-order kinetics.

Formulation Development and Optimization of Sustained Release Microspheres of Acebrophylline

Objectives: Aim of present work is to prepare and evaluate Sustained release microspheres of Acebrophylline for treatment of Asthma.
 Experimental work: In present investigation, attempt was made to prepare sustained release microspheres of Acebrophylline with different polymer ratio using Ionic gelation method. Drug- excipient compatibility studies were performed by FTIR. The best suited Microspheres formulation was found on the basis production yield, entrapment efficiency and in vitro release study. Optimized batch of microspheres (B2) was characterized for FTIR, DSC, and SEM analysis. The drug release data of optimized batch was fitted into different release kinetic models. The optimized batch of microspheres (B2) was subjected for the short term stability study at 40 ± 2°C with RH of 75% for a period of 1 month.
 Results and discussion: There was no interaction found between drug and excipients. Sodium alginate (2%) concentration, Eudragit RS-100 (1:2) ratio gave highest sustainable property and CaCl2 (2.5%) concentration had a good cross linking property. This observation done on the basis of production yield, entrapment efficiency and In vitro release study. The Microspheres prepared from Ionic gelation method had Drug : Eudragit RS100 (1:2), 2 % Sodium alginate and 2.5 % CaCl2 (B2) give 99.2 % drug release over the periods of 12 hr. The drug release from optimized microspheres formulation (B2) follows first order release kinetic. DSC study showed the melting behavior of drug present into microspheres. SEM studies showed that optimized microspheres were spherical and rough surface. Stability study proved that optimized formulation (B2) was stable.
 Conclusion: Drug: Polymer ratio and Volume of CaCl2 had significant effect on % Entrapment efficiency and Drug release. From the Scanning Electron Microscopy (SEM) study observed that microspheres was spherical and rough surface. Non Fickian diffusion was the mode of drug release from Acebrophylline- loaded microspheres. After stability study no physical changes & almost same drug release was observed in microspheres. Hence, the formulation B2 was stable.

DEVELOPMENT AND EVALUATION OF MEDICATED CHEWING GUM OF RALOXIFENE HYDROCHLORIDE

In this study we formulate Raloxifene hydrochloride, edicated chewing gum to overcome first pass metabolism of it so bioavability increase of drug. We take polyvinyl acetate as chewing gum base. Aspartame, mannitol and sucrose as sweetener. Glycerin as a plasticizer. Beta-cyclodextrine as solubility enhancer and taste masking agent. First we evaluate the API by its melting point after we derived its calibration curve. After this we select proper ratio of Beta-cyclodextrine and API. After we study drug and excipients compatibility by using FTIR. XRD study perform for API and formulation. After we formulate our formulation and perform post-evaluation study like hardness, weight variation, % drug content and % drug release. From all formulation F5 formulation shows best % drug release and % drug content. After we perform stability study for our formulation and after study no major change show in formulation. And in last we perform buccal permeability study. On basis of all study results we can say that our formulation is successfully formed.
 Keywords: Raloxifene hydrochloride, Medicated chewing gum, Buccal permeation, Osteoporosis.

Development, Characterization and Comparative Phar-macokinetic Evaluation of Ritonavir Nanosuspension, with a Model Nanoemulsion and Coarse Suspension for Improved Oral Delivery

Ritonavir (RV) is an antiretroviral drug, classified as BCS class II pharmaceutical active.It has limited bioavailability due to poor aqueous solubility and first pass metabolism. The purpose of this investigation was to develop optimal nanosuspension and to compare with a model nanoemulsion of RV for improved oral delivery. DSC studies showed good compatibility of excipients with drug. Nanosuspension was prepared by high pressure homogenization, while nanoemulsion was prepared by hot homogenization followed by ultrasonication. All prepared RV formulations were characterized and optimal system was selected and in vivo evaluated. Nanosuspension (F1) formulation containing 0.5% SLS showed homogeneity with least particle size was optimized and compared with coarse (powder) suspension. SEM studies on lyophilized nanosuspension revealed the absence of needle shaped drug crystals, indicating the loss of crystallinity. Prepared a model lipid nanoemulsion. It was having the size, PDI, ZP, EE and assay of 193.14 ± 12.66nm, 0.311 ± 0.04, -27.6 ± 1.184mV, 90.79 ± 0.319% and 99.57 ± 1.25% respectively. Next, a comparative pharmacokinetic study of RV nanosuspenison with respect to lipid nanoemulsion and coarse suspension was performed in male wistar rats. The Cmax of nanosuspension was significantly more when compared to that of NE or coarse drug suspension. The tmax was similar in case of both nanodelivery systems and significantly less when compared to that of coarse suspension. About 1.36 and 1.27 fold improvements in relative bioavailability (BA) of ritonavir via lipid nanoemulsion and nanosuspension were found when compared to coarse suspension. The study results revealed nominal but nonsignificant difference in oral bioavailability for the two nanodelivery systems. Taken together, this study confirmed the potential of nanosuspension and nanoemulsion systems in improving the bioavailability of ritonavir.

Formulation and Evaluation of Ketoprofen Using β-Cyclodextrin Capped Silver Nanoparticles

The objective of the study was to develop silver nanoparticles loaded with Ketoprofen (Ag-KP) for increasing the drug solubility and thereby its bioavailability. Ag-KP were prepared by the solvent evaporation method using β-Cyclodextrin as a biodegradable polymer. Different formulations of Ag-KP were characterized for the drug entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), particle size analysis, X-ray diffraction studies (XRD), scanning electron microscopy (SEM) and in-vitro dissolution studies. The optimized formulation (F6) has shown an average particle size of 167.8 ± 3.46 nm,zeta potential of -23.7 ± 1.46 mV. FTIR revealed that the drug showed good excipient compatibility. XRD studies showed that the drug has changed from crystalline to amorphous state. In all formulations, F6 formulation (optimized) exhibited high drug entrapment efficiency (∼93%). SEM studies indicated the shape of Ag-KP was roughly spherical with smooth surface. In vitro dissolution studies showed that Ag-KP from F6 formulation was 94.3 ± 4.9% but for the marketed formulation, it is only 84.6 ± 3.7% in 12 hours and F6 was found to be found stable for three months at both refrigerated and room temperature (RT).

Optimization and Characterization of Brimonidine Tartrate Nanoparticles-loaded In Situ Gel for the Treatment of Glaucoma

ABSTRACT Purposes: The present study aimed to develop brimonidine tartrate loaded poly(lactic-co-glycolic acid) acid vitamin E-tocopheryl polyethylene glycol 1000 succinate (BRT-PLGA-TPGS) nanoparticles in thermosensitivein situ gel to improve mucoadhensive properties and drug holding capacity for the better management of glaucoma. Methods: Nanoparticles was optimized by means of Box-Behnken Design (BBD). The formulations were prepared using various concentration of PLGA (0.1–0.4% w/v) and TPGS (0.3–0.5% w/v). The analytical data of fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and transmission electron microscopy (TEM) depicted the drug excipients compatibility and confirmed the nanoparticles. Nanoparticles incorporated gel was evaluated for transcorneal permeability, gelation time, gelling temperature, and rheological studies. In addition, in vitro, transcorneal permeation drug release studies and intraocular pressure (IOP) for optimized gel was also performed. Biocompatibility of formulations was investigated in rabbit model. Results: The drug loaded nanoparticles exhibited 115.72 ± 4.18 nm, 0.190 ± 0.02, −11.80 ± 2.24 mV and 74.85 ± 6.54% of mean size, polydispersity index (PDI), zeta potential and entrapment efficiency (% EE), respectively. As compared to marketed eye drop, the sustained and continuous release BRT release from Poloxamer-based in situ gel was 85.31 ± 3.51% till 24 h. The transcorneal steady-state flux (136.32 μg cm−2 h−1) of optimized in situ gel was approximately 3.5 times higher than marketed formulation (38.60 μg cm−2 h−1) flux at 4 h. The optimized formulation produces 3 fold greater influences on percentage reduction of IOP (34.46 ± 4.21%) than the marketed formulation (12.24 ± 2.90%) till 8 h. Conclusion: The incorporation of optimized BRT-PLGA-TPGS nanoparticles into a thermosensitivein situ gel matrix to improve precorneal residence time without causing eye irritation and also serve the sustained release of BRT through cornea for effective management of glaucoma.

Attenuation of lipid levels in triton induced hyperlipidemia rats through rosuvastatin calcium nanoparticles: Pharmacokinetic and pharmacodynamic studies

The aim of this research was to study the effect of marketed tablet (Crestor®) powder suspension (MTPS) and nanoparticle formulation of rosuvastatin calcium (RC) on the pharmacokinetic (PK) and pharmacodynamic (PD) parameters in hyperlipidemia rats. The hyperlipidemia is induced by intraperitoneal injection of Triton-X-100 in 0.9 %w/v saline solution. The marketed tablet was dispersed into suspension. The RC loaded nanoparticles (RC-NPs) are prepared by homogenization method. The prepared RC-NP formulation was characterized for size, drug excipient compatibility and crystallization by differential scanning calorimeter (DSC), morphology by SEM, stability at room temperature, in-vitro dissolution and in-situ absorption in rats. Further, the pharmacokinetic and pharmacodynamic studies were conducted in hyperlipidemia rats. The size of the RC-NP formulation was found to be 183.4 ± 4.5 nm and to be nearly spherical by SEM. DSC studies revealed that no interaction and RC converted to amorphous form in RC-NP formulation. RC-NP formulation was physically and chemically stable over two months at room temperature. The drug release was found to be 25.8 ± 2.5 and 89.96 ± 2.8 % in five mins, respectively from MTPS and RC-NP formulations. The Peff of MTPS and NP of RC was 1.8 ± 0.2 × 10−5 and 2.7 ± 0.3 × 10-5 cm/s, respectively. From the PK studies, the enhancement in the oral bioavailability was found to be 2.4-folds when compared to MTPS formulation and statistically significant (p < 0.05). PD study of RC-NP formulation in hyperlipidemic rats exhibited decrease in lipid profile for 24 h, while MTPS exhibited a decrease in lipid profile for 12 h. Therefore, the results conclusively demonstrate the nanoparticles of RC showed significant enhancement in the PK and PD parameters.

Evaluation of spironolactone compatibility with magnesium stearate and other lubricants in paediatric formulation using thermal and nonthermal techniques

Spironolactone is a potassium-sparing diuretic used as treatment for several diseases such as bronchopulmonary dysplasia, precocious puberty, hypertension or primary aldosteronism in child population. Because of the lack of paediatric formulations in the market, two types of solid oral formulation containing 2.5 and 10 mg of spironolactone were developed. During stability studies, excessive degradation was observed. As presented in this work, the degradation of spironolactone was linked to a drug excipient interaction between spironolactone and magnesium stearate via alkaline hydrolysis degradation pathway. In order to help the re-formulation with another lubricant, a complete drug excipient compatibility study was performed using thermal analysis techniques associated with chromatographic quantification of the drug after an isothermal stress testing. Spironolactone presents physicochemical incompatibilities with sodium benzoate, sodium stearyl fumarate, PEG 8000, PEG 20,000 and stearic acid. But no degradation was observed with PEG 20,000 and stearic acid indicating chemical compatibility. In total, talc, stearic acid and PEG 20,000 could be used for re-formulation of spironolactone paediatric drug.

Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study.

BackgroundPhytostanols are naturally occurring compounds that reduce blood cholesterol levels significantly. However, their aqueous insolubility poses formulation challenges.AimTo formulate and characterize solid lipid nanoparticle carriers for phytostanol esters to enhance the bioavailability of phytostanols.MethodsPhytostanol ester solid lipid nanoparticles were formulated by the microemulsion method. They were characterized for particle size distribution, polydispersity index, shape, surface charge, entrapment efficiency, stability, chemical structure, and thermal properties. The uptake of the formulation by cell lines, HepG2 and HT-29, and its effect on cell viability were evaluated.ResultsThe formulation of solid lipid nanoparticles was successfully optimised by varying the type of lipids and their concentration relative to that of surfactants in the present study. The optimised formulation had an average diameter of (171 ± 9) nm, a negative surface charge of (−23.0 ± 0.8) mV and was generally spherical in shape. We report high levels of drug entrapment at (89 ± 5)% in amorphous form, drug loading of (9.1 ± 0.5)%, nanoparticle yield of (67 ± 4)% and drug excipient compatibility. The biological safety and uptake of the formulations were demonstrated on hepatic and intestinal cell lines.ConclusionPhytostanol ester solid lipid nanoparticles were successfully formulated and characterized. The formulation has the potential to provide an innovative drug delivery system for phytostanols which reduce cholesterol and have a potentially ideal safety profile. This can contribute to better management of one of the main risk factors of cardiovascular diseases.

Polymeric Films Containing Tenoxicam as Prospective Transdermal Drug Delivery Systems: Design and Characterization

The administration of drugs via transdermal therapeutic systems has become an attractive form of therapeutic approach, considering its advantages and the high patient compliance achieved, making them a viable alternative, especially in the treatment of chronic diseases. The purpose of our study was the development of polymer-based films containing tenoxicam (TX) and the analysis of dissolution kinetics. Auxiliary substances represent an important part of pharmaceutical forms, so during the first stage, TX and excipient compatibility were verified. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analyses were performed on TX and on physical mixtures of TX-HPMCE5 and TX-HPMC15kcP. Three polymeric films of TX (TX1, TX2, and TX3) were prepared using a solvent evaporation technique. Release studies were done at 32 °C ± 1 °C with a Franz diffusion cell. The results of the DSC and FT-IR analyses demonstrated the compatibility of the active substance with the two matrix-forming polymers. The results obtained in the release studies of TX from the proposed polymeric films suggested a pH-dependent behavior in all three polymeric films. At pH 5.5, flux values were between 8.058 ± 0.125 μg·cm−2·h−1 and 10.850 ± 0.380 μg·cm−2·h−1; and at pH 7.4, between 10.990 ± 0.2.490 μg·cm−2·h−1 and 53.140 ± 0.196 μg·cm−2·h−1. The Korsmeyer–Peppas model described a non-Fickian transport mechanism. The n values varied between 0.63–0.7 at pH 5.5 and 0.73–0.86 at pH 7.4, which suggested a diffusion depending on the matrix hydration and polymer relaxation.

Invitro Designing of Fluvastatin Chrono Formulation

The objective was to improve fluvastatin prescribed pulsatile release formulation to get the disintegrative and ruptured lag-time mechanism with a fixed time delay which matches the chronotherapeutics (hypercholesteroidal disorder). Pre formulation studies UV, FTIR (Drug excipient compatibility), solubility studies and flow properties were evaluated for blend and drug. All the values were within the limit. 12 core tablets were prepared with two novel disintegrants, i.e. ludiflash, lycoat in different concentrations after doing the post-compression parameters &amp; drug release F8 was optimized &amp; then coated with PH sensitive polymers HPMC K200M &amp; Ethylcellulose in different concentrations. An evaluation was carried out for all six formulations, and all the values were within the limit. Based on In-vitro dissolution studies, swelling index and rupture test C5F8 is optimized and compared with the marketed product for 10 hours. As per the ICH guidelines optimized formulation (C5F8), stability tests were conducted for three months and was found to be stable. Optimized formulation (C5F8) contains 3:2 polymers (HPM K200M: Ethylcellulose) demonstrates an outstanding pulsatile drug delivery relative to the branded version (Lexcol XL) compared to all other formulations.

Porous Polymeric Carrier System for Modified Drug Releaseof Boswellic Acid

Microsponges being the polymeric drug delivery systems consist of porous microspheres that can entrap a wide range of active ingredients. Boswellic acid is a pentacyclic triterpenoid having anti-inflammatory, anti-hypertensive, anti-cancer activities. The aim of the study was to develop, characterize and formulate microsponge delivery for topical application. The Microsponges were prepared by quasi emulsion solvent diffusion method using QbD approach. Drug excipient compatibility study was carried out by FT-IR, DSC and XRD. The prepared Microsponges were further evaluated for its physicochemical properties by scanning electron microscopy (SEM), photomicroscopy, transmission electron microscopy (TEM), particle size, zeta potential, and porosity analysis. The optimized Microsponges were incorporated into gel base formulation and evaluated for in-vitro drug release, dissolution studies and ex-vivo permeability studies. Further, microsponge formulations, subjected for animal studies for skin irritation test and clinical efficacy. The present study confirmed the formation of Microsponges of Boswellic acid. It also proves the sustained release of drug through microsponge formation.

Healing efficacy and dermal toxicity of topical silver nanoparticles-loaded hydrogel in Sprague–Dawley rats

Traumatic wounds are the wounds that damage both the skin and the underlying tissues. Bacterial load in wounded tissue triggers elongation of the inflammation phase of wound healing. In case of excessive inflammation, the wound may undergo delayed healing that can lead to complications such as sepsis or amputation. In the present work, a hydrogel using green-synthesized silver nanoparticles (AgNPs) was synthesized and characterized in terms of homogeneity, viscosity, spreadability, excipient compatibility, etc. The hydrogels containing different percentages of AgNPs were tested for healing efficacy in full-thickness excision wound model in adult female Sprague–Dawley (SD) rats. Safety study of hydrogels was performed in SD rats as per the OECD guideline 410. The prepared hydrogels were stable for over 3 months and remain intact on parameters such as homogeneity, pH balance, good spreadability, and extrudability. Healing efficacy study showed that an increased amount of AgNPs in hydrogel enhanced wound contraction over 100% with increased tensile strength and dense aligned collagen fibers in treated wound tissues as compared to standard (silver sulfadiazine), placebo, and sham groups. Dermal toxicity studies showed that there were no signs of irritation, inflammation, and edema on the dorsum of SD rats. Besides, there was no local and systemic toxicity in hydrogel-treated groups.

Compatibility by a Nonisothermal Kinetic Study of Azathioprine Associated with Usual Excipients in the Product Quality Review Process

Azathioprine is an immunosuppressive drug for several inflammatory disorders. Due to its clinical relevance, to explore the solid-state properties for excipient compatibility in the product quality review process is essential. Fourier transform infrared spectroscopy, powder X-ray diffraction and thermal analysis (thermogravimetry/derivative thermogravimetry (TG/DTG), differential thermal analysis (DTA), and differential scanning calorimetry (DSC)) were applied. The compatibility studies evidenced that starch pregelatinized, colloidal silicon dioxide, and talc are fully compatible with azathioprine. However, stearic acid, magnesium stearate, and mannitol are incompatible after heat supply at temperatures easily reached by industrial processing. The nonlinear Vyazovkin isoconversional treatment performed the kinetic study of the thermal degradation. The activation energies were determined to clarify the influence of each excipient on the thermal drug stability, an essential procedure in the pharmaceutical development, and all over the commercial live span, in Good Manufacturing Practices.

Drug Excipient Compatibility, Development and Preliminary Clinical Studies of Tizanidine Hydrochloride Floating Drug Delivery System

The objective of this investigation was to develop formulation of floating matrix tablets of tizanidine HCl to prolong the gastric residence time by using hydroxy propyl methyl cellulose (HPMC K15M) or xanthan gum as sole release retardant and to check the clinical response. The drug-excipients compatibility studies were conducted using DSC and also by visual observation. Incorporation of NaHCO3 in the formulation resulted incompatibility with drug and therefore, the composition was modified by replacing NaHCO3 with CaCO3 in remaining formulations. Floating matrix tablets of tizanidine were developed by direct compression method and the developed ten formulations exhibited satisfactory physicochemical characteristics and in-vitro buoyancy. Formulation (F9) was selected as optimized formulation based on physicochemical characters, in-vitro buoyancy and drug release, and was used in in-vivo radiographic studies in human volunteers by incorporating BaSO4. In radiographic studies, the gastric retention time of floating tablets was found to be 4 ± 0.86 h (n=3). Optimized floating tablets (F9) were used to know the clinical effects in patients suffering from spasticity under the observation of clinician. The optimized tizanidine HCl floating matrix tablets were developed and found to have gastric retention behaviour in stomach and further were found to have good clinical effects in patients suffering from spasticity during preliminary clinical studies.

Preformulation characterization towards design and development of dexibuprofen loaded nanoparticles

The intention of the current study was to investigate the Physico-chemical characteristics of Dexibuprofen loaded nanoparticles. Dexibuprofen is an NSAID - non-steroidal anti-inflammatory drug intended for the treatment of rheumatoid arthritis related symptoms. In current market trends, the tablets and capsule dosage forms captures major market contribution. A systematic evaluation of physico chemical characteristics of the drug powder, it’s characteristics was performed as a basic step at the start of formulation development of the dosage form. The formulation development approach is decided based on the above data. Dexibuprofen nanoparticles was developed by an Ionotropic pre gelation technique comprising Chitosan, Calcium chloride and Sodium alginate as coating material. The preformulation evaluation of Dexibuprofen and it’s compatibility with selected excipients was performed to design an appropriate strategy for the development of Dexibuprofen modified release nanoparticles. The parameters like melting point, pKa, solubility, dissolution and assay method development, solid state stability, solution stability, flow properties, bulk density, microscopical assessment, entrapment efficiency, excipients compatibility, and nanoparticles release profile were evaluated. The results of this study, along with the experimental values, will be discussed in detail.

Application of quality by design paradigm in the design of muco-adhesive extended release film for oral ulcer

The present study deals with the formulation of mucoadhesive bilayered buccal film of lidocaine hydrochloride and benzydamine hydrochloride for treatment of oral ulcers (aphthous stomatitis). Eudragit-RLPO and Ethyl cellulose were used as film forming polymers and low viscosity grade hydroxyl propyl cellulose as a mucoadhesive agent. Solvent casting method was adopted for film formation. The film was evaluated for content uniformity, tensile strength, folding endurance, swelling, mucoadhesive strength, ex vivo mucoadhesive time and in vitro drug release. The films were characterized for DSC and FTIR. The film showed acceptable film properties and muco-adhesion. The formulation showed predictive drug release, i.e. 80 in 2, 4 and 6 h respectively. In-vitro drug release study revealed that a combination of Eudragit and Ethyl cellulose was required for better control of the drug release. The DSC and FTIR study confirmed drug-drug and drug–excipient compatibility. Keywords: Bilayer film, Eudragit-RLPO, Ethyl cellulose, Muco-adhesion, Extended drug release.