Determination Of Drug Content Research Articles

A Stereolithography-Based Modified Spin-Casting Method for Faster Laboratory-Scale Production of Dexamethasone-Containing Dissolving Microneedle Arrays

Microneedle arrays (MNAs) consist of a few dozens of submillimeter needles, which tend to penetrate through the stratum corneum layer of the skin and deliver hardly penetrating drugs to the systemic circulation. The application of this smart dosage form shows several advantages, such as simple use and negligible pain caused by needle punctures compared to conventional subcutaneous injections. Dissolving MNAs (DMNAs) represent a promising form of cutaneous drug delivery due to their high drug content, biocompatibility, and ease of use. Although different technologies are suitable to produce microneedle arrays (e.g., micromilling, chemical etching, laser ablation etc.), many of these are expensive or hardly accessible. Following the exponential growth of the 3D-printing industry in the last decade, high-resolution desktop printers became accessible for researchers to easily and cost-effectively design and produce microstructures, including MNAs. In this work, a low force stereolithography (LFS) 3D-printer was used to develop the dimensionally correct MNA masters for the spin-casting method. The present study aimed to develop and characterize drug-loaded DMNAs using a two-level, full factorial design for three factors focusing on the optimization of DMNA production and adequate drug content. For the preparation of DMNAs, carboxymethylcellulose and trehalose were used in certain amounts as matrices for dexamethasone sodium phosphate (DEX). Investigation of the produced DexDMNAs included mechanical analysis via texture analyzer and optical microscopy, determination of drug content and distribution with HPLC and Raman microscopy, dissolution studies via HPLC, and ex vivo qualitative permeation studies by Raman mapping. It can be concluded that a DEX-containing, mechanically stable, biodegradable DexDMNA system was successfully developed in two dosage strengths, of which both efficiently delivered the drug to the lower layers (dermis) of human skin. Moreover, the ex vivo skin penetration results support that the application of DMNAs for cutaneous drug delivery can be more effective than that of a conventional dermal gel.

Development of topical silver nano gel formulation of Bixin: Characterization, and evaluation of anticancer activity

ObjectiveSkin cancer refers to the pathological condition characterized by the proliferation of atypical skin cells in an uncontrolled manner. Plant-based products such as bixin although show promising anticancer properties, but maintaining their stability in a formulation is a difficult task. The objective of the research is to formulate a silver nanoparticle gel preparation of bixin and evaluate its anticancer properties. MethodsThe extract from Bixa orellana seed was prepared by hot extraction technique to isolate the active ingredient, bixin. A green synthesis approach was utilized for preparing the silver nanoparticle gel of bixin (BOAgNPs). Characterization of silver nanoparticles was done using FTIR, scanning electron microscopy, compatibility study, homogeneity testing, pH evaluation, and drug content determination. The in-vitro anticancer activity was performed using cell lines (B16F10) and in-vivo by chemical carcinogen (7,12-dimethylbenz (a) anthracene) in mice. ResultsThe BOAgNPs-loaded topical gel was found to be homogeneous (clear orange color) and pH-compatible (pH ≈ 6.66) with the skin. The characterization studies indicated the presence of all functional groups in the formulation. An optimized batch of bixin-nano gel showed about 60% inhibitory effects on B16F10 cell lines (in-vitro activity) when equated with a reference drug, 5-fluorouracil. The in-vivo anticancer study suggested suppression of tumorigenesis and promotion of the healing process with bixin-nano gel application on the skin. ConclusionThe results suggested the promising anticancer property of bixin when formulated in silver nanoparticle gel. The preparation of silver particles nano gel with bixin might provide an effective alternative option for treating skin cancers, provided more research complements the findings of the present study.

Insights into folic acid mixtures compounded with commercially available vitamin syrups

Stability assessments are crucial in determining the shelf-life and quality of compounded pharmaceutical products. Folic acid, an essential B-vitamin, is widely used to prevent and treat folate deficiency-related conditions. However, because of patient-specific demands or customised dose requirements, compounded folic acid syrups are frequently used in pediatric patients. This study aims to examine the stability of compounded folic acid mixtures prepared with some commercially available vitamin syrups. Three commercially available vitamin syrups were utilized as compounding vehicles for folic acid tablets, ensuring a representative sample of products commonly used in compounding practices in hospitals when conventional compounding vehicles are not available. The compounded folic acid mixtures were stored under ambient (21- 25 ºC) and refrigerated conditions (2-8 ºC), to simulate real-life scenarios, and tested using parameters such as, organoleptic characteristics, sedimentation rate, pH, microbial growth and drug content determination at day 7, 14 and 30. The extemporaneous preparations of the compounded folic acid in vitamin syrups generally maintained their physical characteristics over the 30-day study period. However, there was either decrease in folic acid concentration or microbial contamination of the preparations at day 7. Therefore, folic acid compounded in vitamin syrups are generally stable for less than seven days. The data obtained will aid healthcare professionals and compounding pharmacies in decision making concerning the choice of vehicle, compounding practices and strategies to ensure the preparation of wholesome extemporaneous products.

Drug content determination of low-dosed hot-melt extruded filaments using Raman spectroscopy

The aim of this study was to evaluate the suitability of a non-disruptive Raman spectroscopic method to quantify drug concentrations below 5 w% within a polymer matrix produced by hot-melt extrusion (HME). For calibration, praziquantel (PZQ)—polyvinylpyrrolidone-vinylacetat-copolymer (PVP-VA) mixtures were extruded. By focusing the laser light of the Raman probe to a diameter of 1 mm and implementing a self-constructed filament holder, the signal-to-noise (S/N) ratio could be reduced considerably. The obtained Raman spectra show quite high fluorescence, which is likely to be caused by dissolved pharmaceutical active ingredient (API) in the polymer matrix. For content determination, HPLC analysis was conducted as a reference method using the same filament segments. A partial least squares (PLS) model, regressing the PZQ concentrations from HPLC method analysis versus the off-line collected Raman spectra, was developed. The linear correlation for a suitable extrusion run for the production of low-dosed filaments (extrusion 1, two kneading zones) is acceptable (R 2 = 0.9915) while the correlation for a extrusion set-up with low miscibility (extrusion 2; without kneading zone) is unacceptable (R 2 = 0.5349). The predictive performance of the calibration model from extrusion 1 is rated by the root mean square error of estimation (RMSEE), which was 0.08%. This calibration can now be used to validate the content of low-dosed filaments during HME.

Preparation of Tamsulosin Hydrochloride-Loaded Mucoadhesive In Situ Gelling Polymeric Formulation for Nasal Delivery in Geriatrics.

This study aimed to prepare tamsulosin hydrochloride (HCl)-loaded in situ gelling formulation by using hydroxypropyl methylcellulose (HPMC), gellan gum, poloxamer 188, and benzalkonium chloride. Physicochemical evaluation of formulations included determination of pH, viscosity, gelation time, gel strength, drug content, and sterility. In silico study was performed to analyze interactions between polymers, drug, and mucin glycoprotein. In vitro degradation time, drug release, ex vivo mucoadhesion time, permeation, in vivo pharmacokinetics, and stability studies were performed to assess the formulation. Formulations were transparent and displayed acceptable physicochemical attributes. Tamsulosin HCl and polymers interacted via non-covalent interactions. HPMC formed hydrogen bonds, hydrophobic and van der Waals interactions with mucin protein while the drug formed hydrogen bonds only. Gel formulation degraded in simulated nasal fluid within 24 h. In situ gelling formulation showed 83.8 ± 1.7% drug release and remained adhered to the mucosa for 24.5 ± 1 h. A higher (~ 1.85 times) drug permeation was recorded through mucosa within 6 h by in situ gelling formulation when compared to control counterparts (aqueous solution of drug and in situ gelling formulation without poloxamer 188). Nasal administration of tamsulosin HCl by using in situ gelling formulation led to a ~ 3.3 and ~ 3.5 times, respectively, higher Cmax (maximum plasma concentration) and AUCtotal (total area under the curve) than the orally administered aqueous solution. Relative bioavailability of drug delivered by nasal in situ gelling formulation was 3.5 times the oral counterpart. These results indicated that the prepared in situ gelling formulation can act as a promising candidate for systemic administration of tamsulosin HCl.

Propofol Quantification method in Palm Oil Based Nanoemulsion Formula using RP-HPLC

HPLC is one of the methods that is widely used for the routine determination of drug content in a pharmaceutical dosage form. The objective on this research was to develop a simple method to determine the propofol concentration in a new formulation using a palm oil-based nanoemulsion carrier system (NEMS™ MCT/LCT). The method used was reverse phase high performance liquid chromatography (RP-HPLC) using a C18 column with methanol and water (80:20) as the mobile phase and UV wavelength detection was 276 nm. The retention time obtained for the drug in NEMS MCT/LCT was 6.32 min. This was similar to the retention time of the standard. The correlation coefficient value from the calibration curve was 0.9998. The drug contents were 100.90% and 100.24% for the 1% and 2% NEMS MCT/LCT, respectively. The result indicated that the RP-HPLC method used for the analysis of propofol in the palm oil-based emulsion system was able to accurately determine the concentration of the drug.This method is suitable for routine determination of propofol concentration in palm oil-based emulsion formulations.

Preparation and Evaluation of Niosomal Transdermal Patch of Clozapine

Niosomes are the non-ionic surfactant vesicles obtained on hydration of synthetic non-ionic surfactants. These are the promising vehicles for effective transdermal drug delivery. The present research work was aimed to develop niosomal-based transdermal Clozapine patch containing a stable formulation with improved drug permeation. Niosomes were prepared by solvent casting method. All the formulations were evaluated for vesicle size, zeta potential and percent entrapment efficiency. All the patches were then characterized for thickness, folding endurance, drug content determination, Flatness, and in vitro permeation studies. F3 formulation having optimum vesicle size (2.6m), highest zeta potential (-32.56mV) and maximum percent entrapment efficiency (98.09%) was selected as optimized formulation. The transdermal patch was prepared using solvent casting method from the optimised niosomes formulation F3 formulation. The prepared optimised niosomes F3 formulation were loaded into the patch formulation. Patches loaded with niosomes (F3NT3) showed 95.78 % cumulative amount of drug permeated. The optimized formulation (F3NT3) followed first order release kinetics.

Ultrasensitive SERS substrate for label-free therapeutic drug monitoring of chlorpromazine hydrochloride and aminophylline in human serum

Surface-enhanced Raman spectroscopy (SERS) has been widely used in the field of therapeutic drug monitoring (TDM) because of its powerful fingerprinting capability. In this paper, we used an in situ synthesis method to anchor Ag nanoparticles (AgNPs) on the surface of MIL-101(Cr) to obtain MIL-101(Cr)@Ag. Owing to the large specific surface area and ultra-high porosity of MIL-101(Cr)@Ag, we developed a method for the determination of chlorpromazine hydrochloride (CPZ) and aminophylline (AMP) in human serum by using it as a solid-phase extraction sorbent and SERS substrate. The label-free TDM-SERS method was able to evaluate the levels of CPZ and AMP in serum samples with detection limits as low as 8.91 × 10-2µg/mL and 3.4 × 10-2µg/mL, respectively. In addition, influencing factors including sample solution pH, AgNO3 concentration, drug adsorption time, and the amount of sample solution were optimized. This protocol provides a new method with good selectivity, stability, reproducibility, homogeneity, and sensitivity for the determination of small-molecule drug content in serum samples. This label-free TDM-SERS method will help to achieve rapid individualized dosing regimens in clinical practice and has potential applications in the field of TDM.

Formulation and Evaluation of Antidiabetic Chocolate by using Guava Leaves and Mulberry Fruits

The chocolate is product which love every age person to eat but due to health issues like obesity, high blood pressure, coronary artery disease, diabetes etc. doctor restrict patient to take chocolate. So, objective of present research was to formulate the medicated chocolate keeping note of health issuesto prevent the Diabetes and make patient convenient to eat chocolate. Psidium Guajava is synonyms Guava leaves have high levels of antioxidants and vitamins which also helps to lower blood sugar levels. Chocolate formulation contained Guava leaves powder, dark chocolate, cocca butter, coffee, stevia sugar and evaluated parameters are general appearance, dimension, hardness, blooming test, drug content determination, physical stability etc.

Biodegradable Polymeric Pharmaceutical Nanoemulgel Coloaded with Eucalyptol‐Lornoxicam: Fabrication and Characterizations for Possible Better Pain Management

Nanoemulgels are considered as potential and ideal drug delivery systems for the transdermal administration of poorly soluble drugs like lornoxicam. Their intrinsic characteristics, such as small globule size as well as excipient type, make transdermal passage of the drug easier. The current study was aimed at developing nanoemulgel based formulation of lornoxicam coloaded with eucalyptol to enhance drug skin permeation and bioavailability in order to promote therapeutic outcome in appropriate time. High shear homogenization technique was utilized to develop optimized lornoxicam encapsulated nanoemulsion followed by its conversion into nanoemulgel formulation by the addition of 1% Carbopol 940 as gelling agent. Different characterization tests were performed on optimized formulation such as surface charge, particle size and size distribution, viscosity, spreadability, pH, drug content determination, drug entrapment efficiency, in vitro drug release, and drug permeation analysis. The optimized formulation had globule size of 143.7 ± 2.18 nm. The results of drug entrapment efficiency, in vitro drug release, and skin penetration experiments were found satisfactory. Based on the formulation type, permeability parameters such as permeability constant (Kp), enhancement ratio (Er), and steady state flux (Jss) revealed greater values and satisfactory outcomes. When compared to other formulations (LRX nanoemulgel and EU nanoemulgel), the LRX‐EU nanoemulgel formulation produced improved skin permeation profile (flux, 189.63 ± 7.68 μg/cm2/h; permeability coefficient, 2.09 ± 0.067 cm/h; and ER, 4.274). This work clearly proved that lornoxicam coloaded with eucalyptol nanoemulgel formulations could be developed to generate stable drug delivery systems. Thus, LRX‐EU NEG formulation seems promising in terms of physicochemical properties, enhanced bioavailability, and high skin penetration profile as compared to LRX NEG formulation.

FORMULATION AND INVITRO EVALUATION OF PRAZOSIN HYDROCHLORIDE UNFOLDING TYPE GASTRO RETENTIVE FILM

The present work is based on the formulation and In-vitro evaluation of a gastroretentive mucoadhesvie based drug delivery system containing prazosin hydrochloride for controlled release. It consists of a drug loaded polymeric film folded into a hard gelatin capsule. After administration film unfolds and its swelling and bioadhesion to the gastric mucosa. Prazosin hydrochloride, a histamine H2 receptor antagonist used for gastroesophageal reflux disease (GERD), duodenal ulcer and gastric ulcer. Prazosin hydrochloride absorbed only in the initial part of gastro intestinal tract (GIT) and has less bioavailability. Thus by retaining the drug in the gastric region improves its bioavailability. Films were prepared by solventcasting method using HPMC K4M, and Carbopol 971P NF as polymers and PEG 400 as the plasticizer. The prepared film were evaluated for various parameters such as film thickness, folding endurance, uniformity of weight, surface pH, determination of drug content, moisture content, swelling index, In-vitro mucoadhesive study retention time, In-vitro unfolding behavior and In-vitro drug release studies and drug release kinetics. Differential scanning calorimetry revealed there were no polymorphic changes in drug as well as polymers during the formulation of polymeric film. Optimized formulation showed 99.02 % drug release at the end of 12 hrs and it follows the Korsmeyer-peppas kinetics model of drug release. Keywords: Gastroretentive mucoadhesive film, Solvent casting method, Prazosin hydrochloride

Chemometrically Assisted Optimization of Pregabalin Fluorescent Derivatization Reaction with a Novel Xanthone Analogue and Validation of the Method for the Determination of Pregabalin in Bulk via a Plate Reader.

Quantitation of chromophore-free analytes is always a challenge. To this purpose, derivatization of the analyte constitutes a common strategy, leading to a product with a strong signal. In the current study, a novel xanthone analogue was utilized for the first time for the derivatization of pregabalin, a model analyte with a primary amine moiety that lacks a chromophore. The fact that only the xanthene-based derivative, formed after the derivatization reaction fluoresces, enables avoiding its chromatographic separation from the reagent and thus reducing the analysis time of a series of samples in 1–2 min via a plate reader. The reaction conditions were optimized via a central composite design (CCD), with fluorescence signal as the measure of the yield. The following factors that affect the derivatization reaction were chosen: (a) temperature, (b) reaction time, and (c) triethylamine solution volume used to drive the reaction to completion. After the identification of the optimal conditions, the method was validated according to ICH guidelines, using a fluorescence plate reader for signal measurement (λex = 540, λem = 615 nm). Finally, the newly developed high-throughput method was applied to the determination of drug content in pregabalin bulk.

Ophthalmic release of in situ gel Ciprofloxacin HCl based on combination of Hypromellose and HPC

The development for ophthalmic delivery was purposed to achieve optimum drug loading for ocular therapeutic benefits. An adequate dose of the drug is needed to absorb in the conjunctival sac to take effect. In situ gel preparation was expected to provide these needs with the polymer aid that makes the droplets suddenly coagulate in the eye area to maintain the drug dose. The in situ gel dosage form is desired to overcome the poor bioavailability of conventional ciprofloxacin HCl eye drops on the market. Thus, this work was studied using two cellulose polymers such as hydroxyl propyl cellulose (HPC) and hydroxypropyl methylcellulose (HMPC) as a gelling forming agent. The effect of the in situ ophthalmic quality of the gel due to the two individual polymers separately and their combined use was investigated. The in situ gel quality includes the ability of gel-forming under the influence of varying temperature and stirring frequency difference (as a rheological study) was tested together with the drug release model model. Other ophthalmic preparation quality parameters such as clarity, pH measurement, drug content determination, sterility, and antibacterial activity have been evaluated. However, overall in situ gel formulation developed was of better quality compared to the conventional one. Consideration of the choice of cellulose derivative polymer type is seen to affect the quality of controlled release kinetics models.Keywords: Ophthalmic gel, Ciprofloxacin HCl, HPMC, HPC, Drug release kinetics

Synthesis and evaluation of grafted xanthan gum as a drug carrier in developing lornoxicam gel formulations

Background: In the medical and pharmaceutical fields, man has successfully used natural-origin things for millennia. Polymers obtained from plant sources have flashed much consideration in current eras owing to their various pharmaceutical properties, such as gelling agents in gels. Also incorporated in cosmo products, fabrics, dyes, and paper manufacture as binders, diluents, disintegrating agents, thickeners in oral fluids, protective colloids in suspensions, and bases in a suppository. Objectives: Natural polymers are chosen over semisynthetic and synthetic excipients due to their lack of toxicity, low cost, availability, soothing action, and nonirritant nature, as well as their ability to undergo a variety of chemical modifications. However, they have some drawbacks, including microbial contamination, lot to lot variation, reduced viscosity throughout storage, inappropriate mechanical properties, low storage, and an uninhibited rate of hydration. Current research work aims to chemically modify xanthan gum and study its impact on the formulation of topical gels. Materials and Methods: Chemical modification of xanthan gum is conceded by using a thiol-esterification reaction with thioglycolic acid (TGA) in the presence of hydrochloric acid. Microwave irradiated thiolated xanthan gum was also willing by further irradiation of thiolated xanthan gum by microwave using 750 W frequency. Topical drug delivery of lornoxicam release applications of thiolated and microwave irradiated xanthan gum are comparatively evaluated with pure xanthan gum polymer by formulating gel incorporated lornoxicam as a drug. Results: The physical properties of gel-like physical evaluation and viscosity results are within official limits. Formation of gel with idyllic properties. Determination of drug content, spreadability, and extrudability of modified xanthan gum was high compared with native xanthan gum. In vitro drug release study showed that prepared gel sustains the drug release for 24 h. Conclusion: Thiolation and irradiated xanthan gum sustain the release of lornoxicam over a prolonged period and might be a promising lornoxicam carrier in topical drug delivery to enhance antinociceptive and anti-inflammatory efficiency.

Formulation Development and Evaluation of Colon Targeting Nanosponges of Deflazacort Using Box Behnken Design

Deflazacort is a glucocorticoid that is often used as an anti-inflammatory and immunosuppressant for patients suffering from Inflammatory Bowel Disease such as ulcerative colitis (UC) and Crohn's disease (CD). IBD is difficult to manage, and the most difficult issue for doctors is the recurrence. There are several regulated and colon focused medication delivery devices available for therapy, however they have a low success rate. The goal of this work was to create nanosponges loaded with deflazacort using the quasi-emulsion solvent diffusion technique using Eudragit S-100 and to investigate the influence of process factors on response using the Box-Behnken design. The effect of three independent parameters, Eudragit S100, PMMA, and PVA, on two dependent responses, particle size and percent drug entrapment, was investigated. Using the Box-behnken design, seventeen nanosponge formulations were created using the quasi-emulsion solvent diffusion technique and Eudragit S-100 (0.2 percent to 0.5 percent w/v), PMMA (0.2 percent to 0.5 percent w/v), and PVA (0.5 percent -1.5 percent w/v). Particle size, percent drug entrapment, shape and surface morphology, drug content determination, and in vitro drug release behaviour were all evaluated in the nanosponge formulations. The generated nanosponge was virtually spherical in form and spongy in character, with particle size 170.45 nm and a drug entrapment percentage of 73.42 percent. Over a 24-hour period, in vitro drug release of optimised formulations was shown to have a maximum drug release of 90.33.3 percent in colonic fluid with 4 percent w/v caecal content. The observed values of several assessment parameters were found to be in close agreement with the projected values using the Design expert programme. The nanosponge formulation obtained using Eudragit S-100 in low concentration, optimum concentration ratio of eudragit: PVA along with low stirring speed showed desired features. The mathematical models were further designed to develop nanosponge with required characteristics.

Development of Topical Nanoemulgel Using Combined Therapy for Treating Psoriasis.

This study focuses on the development of topical formulation of methoxsalen using Babchi oil as formulation component that can be applied at body surfaces providing sustained delivery and enhanced penetration of methoxsalen leading to significant epidermal localization and better anti-psoriatic activity. The combination of psoralens, that is, methoxsalen (synthetic) and Babchi oil (natural) has been developed into nanoemulgel formulations. A total of four nanoemulsion formulations was developed using Babchi oil as oil phase and Tween 80 as surfactant by high-pressure homogenization method. The prepared nanoemulsions were characterized for entrapment efficiency, mean droplet size, and zeta potential. Based on characterization results, the optimized nanoemulsion formulation(s) were incorporated into the carbopol gel base to make a nanoemulgel. The prepared nanoemulgel formulations were analyzed for pH, drug content determination, spreadability, viscosity, ex vivo skin permeation, and in vivo studies. The nanoemulsions showed droplet size between 51.3 and 146.7 nm, entrapment efficiency of 92.76%-98.10%, and zeta potential of -28.1 to -54.89 mev. The nanoemulsions showed varied in vitro drug release. In ex vivo skin permeation, nanoemulgel (NG2) showed increased penetration and localized accumulation of methoxsalen across the skin compared with plain gel. Ex vivo results were substantiated by in vivo results showing significant amelioration of hyperproliferative skin symptoms. The promising results suggested that nanoemulgel system is a suitable carrier for the topical delivery of methoxsalen-Babchi oil.

FORMULATION AND EVALUATION OF FLOATING DRUG DELIVERY SYSTEM FOR HYDRODYANAMICALLY BALANCED SYSTEMS OF CURCUMIN TABLET TO TREAT STOMACH ULCER

The present work focuses on formulation and evaluation of floating drug delivery system for hydrodyanamically balanced systems of curcumin tablet to treat stomach ulcer. Floating drug delivery tablets were designed and the present study focused on the manufacture of FDS using various polymers such as HPC and HPMC K15 and H. Its efficacy in reducing ulcers due to pylori was evaluated. Floating drug delivery tablets were characterized for their weight variation, stiffness, stability, drug content determination, dissolution, in-vitro dissolution studies, IR, floating interval time, inflammation studies, and erosion studies. The developed curcumin floating tablet system is a promising floating drug delivery system for oral continuous administration of curcumin.

Particle Engineering and Spray Drying Process designing for Solubility Enhancement of Lopinavir

To improve the solubility enhancement of solid dispersion of Lopinavir by spray-drying by adding the Soluplus as polymer that is compatible with Lopinavir, was evaluated and the process used for preparation of Spray dried solid dispersion was validated and the 1:3 ratio used for preparation of solid dispersion. Dissolution tests were carried out on several spray dried solid dispersion of Lopinavir and physical mixture. The solid dispersion characterized by DSC, XRD, % Entrapment Efficiency, solubility study, drug content determination, practical yield, dissolution studies. Keyword: Lopinavir, Soluplus, Spray Drying Technique, Dissolution studies

FORMULATION AND EVALUATION OF FLOATING IN SITU GEL OF OMEPRAZOLE MAGNESIUM FOR ORAL DRUG DELIVERY SYSTEM

Objective: Omeprazole magnesium is indicated for the treatment of erosive esophagitis associated with gastroesophageal reflux disease. It is one of the highly prescribed proton pump inhibitor in the management of peptic ulcer diseases. The therapeutic concentration of a drug in blood can be maintained for a prolonged period of time by administering it in the form of in situ floating gel dosage form. Omeprazole magnesium undergoes degradation at a low pH of the esophagus and stomach; it is therefore given as in situ gel, so, there is minimum contact with acidic pH. Methods: Omeprazole magnesium suspension prepared using various polymers and floating agents in varying concentrations. Several evaluation tests including dissolution test to ensure the release of the drug from formulation by in vitro technique, color and homogeneity, in vitro floating duration, in vitro gelling capacity, drug content determination, pH of the formulation, and floating lag time were studied. Results: All formulations demonstrated good Fourier-transform infrared compliance and no interaction between drug, polymer, and other excipients. The study’s findings show that the formulation F6 showed the best results. Conclusion: The developed formulation was a viable alternative conventional solution by virtue of its ability to enhance bioavailability through its longer gastric residence time and ability to sustain drug release as well as the advantage of floating and pH which minimize the degradation of omeprazole magnesium which is easily degraded by acidic environment.

DEVELOPMENT AND CHARACTERIZATION OF DICLOFENAC SODIUM LOADED EUDRAGIT RS100 POLYMERIC MICROSPONGE INCORPORATED INTO IN SITU GEL FOR OPHTHALMIC DRUG DELIVERY SYSTEM

Objective: Purpose of the study to design and formulate Diclofenac sodium (DIC) microsponges. Methods: With varied polymer: drug ratio DIC loaded microsponges were prepared with Eudragit RS100 polymer by quasi solvent diffusion method. Microsponges evaluated for particle size, entrapment efficiency, drug content, in vitro drug release, Fourier Transform Infrared Spectroscopy (FTIR), Differential scanning calorimetry (DSC) and Scanning electron microscopy (SEM). DIC loaded microsponges incorporated into ocular in situ gel to attained controlled release by microsponge and improved residence time by gelling system. Ocular in situ gel evaluated for pH, drug content determination, gelling capacity, in vitro drug release and sterility study. Results: DSER4 microsponge formulation having polymer to drug ratio 1:7 showed satisfactory production yield (68.13%), entrapment efficiency (62.86%), drug content (80.73%), requisite particle size (less than 10 µm) (7.52 µm) and in vitro release 87.94% after 6 h. Selected DSER4 formulation was incorporate into in situ gel. Carbopol 940 forms stiff gel at higher pH so used as a gelling agent, whereas Hydroxypropyl Methylcellulose E4M was used as a viscosity-enhancing agent for the formulation of in situ gel in varied compositions. In situ gel formulation IG4 showed sustained release of 76.92% till the end of 8 h and satisfactory gelling capacity so IG4 further evaluated for sterility test. Rheological studies reveal the sol-gel transition of in situ gel occur at the physiological condition to form stiff gel. Conclusion: Prepared in situ gel formulations showed sustained drug release for a period of 8 h, which is satisfactory for management of ocular pain.