World Journal of Pharmaceutical Sciences

FORMULATION AND INVITRO CHARACTERIZATION OF MACITENTAN SOLID DISPERSION TO FAST DISINTEGRATING TABLETS

T.Mohitha, — 2024-11-20

Macitentan is an endothelin receptor antagonist utilized for the management of pulmonary arterial hypertension to impede disease development.It is a BCS Class II medication. To enhance the biological efficacy of Macitentan, a solid dispersion was formed into an oral disintegrating tablet utilizing PEG 6000, Xylitol, and PVP K30. Solid dispersions of Macitentan were created using several carriers in distinct ratios of drug to carrier (1:1, 1:2, 1:3, and 1:4). The outcomes of the generated solid dispersions of Macitentan using the solvent evaporation method were examined, including solubility, melting point determination, drug content uniformity, and in vitro dissolution investigations.Characterization in the solid state was conducted using several analytical methods, including FT-IR investigations.Ultimately, while evaluating all formulations, formulation (F12) including Macitentan and PVP K30 in a 1:4 ratio demonstrated superior outcomes using the solvent evaporation technique after 60 minutes, achieving maximal drug release; hence, it was designated as the optimal formulation.Fast dissolving tablets were produced from the optimal formulation utilizing several disintegrants at varied concentrations.The pre-compression and post-compression parameters were analyzed, and the findings were presented. All findings fall within permissible limits.The in vitro drug release of the prepared tablets was conducted using a 6.8 pH phosphate buffer. The F12T12 formulation with 50mg of Cropovidone exhibits a drug release of 99.74±1.48% within 20 minutes. The improved formulation adheres to first-order release kinetics.

FORMULATION AND EVALUATION OF RILPIVIRINE NANOSUSPENSION BY NANO PRECIPITATION METHOD

A. Vivek Pavan Kumar — 2024-12-13

The aim of the present work is to develop oral Nanosuspension of Rilpivirine by Nano Precipitation method using various Stabilizers & Surfactant such as β-cyclodextrin, Soluplus, Poloxamer 407, Polyvinyl alcohol, Sodium lauryl sulfate, Polysorbate 80 Various formulation as well as process parameters were optimized in order to achieve desirable size and saturation solubility. Characterization of the prepared Nanosuspension was done with respect to Drug Content, Percentage yield, Entrapment efficiency, Viscosity, Sedimentation volume, Scanning electron microscopy, Particle’s size, zeta potential, dissolution rate, in-vitro dissolution study. Zeta potential value for the optimized formulation (NS12) was found to -4.49 mv which was found to be within the acceptable limits. Average particle size of Nano suspension of optimized formulations (NS12) which is in ratio with Poloxamer 407 was found to be 500.4 nm. From the In vitro studies we can say that formulation NS12 shows best drug release of 98.42±1.27% within 30 minutes whereas all the other formulations didn’t release the drug. The drug release from the Nanosuspension was explained by the using mathematical model equations such as zero order, first order, and equation methods. Based on the regression values it was concluded that the optimized formulation NS12 follows first order kinetics with super case-II transport mechanism and the stability studies shows that the formulation was stability upto 3Months of time period.

FORMULATION AND EVALUATION CARBAMAZEPINE BILAYER TABLET

G.Kumari — 2024-11-20

Gastro-retentive medication delivery methods are extensively utilized to extend the retention of dose forms in the stomach. The floating bilayer tablet formulation provides sustained drug release and extended stomach retention, in addition to the benefits of a liquid oral dose form. This study aimed to formulate and assess floating bilayer tablets of Carbamazepine utilizing various polymers, including Lycoat and Crospovidone as superdisintegrants, and Xanthan Gum and Carbopol 934P as extended-release polymers, alongside additional substances such as Magnesium stearate, Sodium bicarbonate, citric acid, Talc, PVP K30, MCC, and Lactose. The fabricated bilayered tablets were assessed for hardness, weight fluctuation, thickness, friability, drug content homogeneity, and in vitro dissolution experiments. F6(IR) and F12(SR) were identified as the optimum formulations based on many assessment factors. The aforementioned buoyancy measurements indicate that F12 exhibits a greater total floating time compared to the other formulations. Formulations F6 (IR) and F12 (SR) exhibited the highest drug release within the specified timeframe. All formulations underwent drug release kinetics tests, including zero order, first order, Higuchi matrix, and Peppas model equations. The sustained release (SR) formulations exhibited zero order release with a super case II transport mechanism.

FORMULATION AND IN VITRO EVALUATION OF SELEXIPAG CONTROLLED RELEASE TABLETS

Surisetty Sridevi — 2024-12-05

Selexipag has a short biological half-life of 0.8-2.5 hours and having less bioavailability which necessitates multiple daily dosing. Hence the present study was aimed to develop a controlled release formulation of Selexipag to reduce the dose related side effects and to reduce the dosage regimen. The present research project aimed to develop a Control release oral formulation of hypertension drug Selexipag, the present research comprising Selexipag used for the symptomatic relief of pulmonary arterial hypertension. Polymers like HPMC K15 M, Carbopol 940, Pectin and Gellan Gum were used for controlling the drug release, and the polymers are mixed in a predetermined ratio. Totally 12 formulations were prepared and evaluated for pre-compression and post-compression parameters, and all the results were found to be within the limits. From the drug and excipients compatibility studies (FT-IR) it was confirmed that the drug and excipients used weren’t have any interactions. The in vitro dissolution studies revealed that the F9 formulation containing 6mg of Pectin controls the drug release up to 12 hours. So Pectin containing F9 formulation was considered to be suitable for the formulation of Selexipag controlled release tablet and the drug release kinetics revealed that the F9 formulation shows zero order kinetics with super case- II transport mechanism.

QUALITY EVALUATION OF NYCTANTHES ARBOR-TRISTIS EXTRACTS BY UV-VIS SPECTROSCOPY AND HIGH-PERFORMANCE THIN-LAYER CHROMATOGRAPHY TECHNIQUES

B. Sandhya Rani — 2024-11-20

Nyctanthes Arbor-tristis is one of the most useful medicinal plants in India. Each part of the plant has some important medicinal value and is thus commercially exploitable. The popular medicinal use of this plant is anti-inflammatory, anti-pyretic, anti-viral, anti-bacterial, anti-allergic and diabetes control and it is used as several diseases. The present research is to isolate plant pigments by different extraction techniques and to focus on the identification and determination of the purity, quality, quantity by using UV-Visible spectroscopy and High performance thin-layer chromatography technique. From the results obtained by the above analytical techniques it is observed that Soxhlet extraction technique showed better results in HPTLC when compared to masceration technique.

FORMULATION AND IN VITRO EVALUATION OF EZOGABINE ORAL THIN FILMS

Surisetty Sridevi — 2024-12-05

Fast dissolving drug delivery system offers a solution for those patients having difficulty in swallowing tablets/capsules. The present research work is to develop oral thin films of Ezogabine by using solvent casting method. Oral thin films were developed by using various super disintegrants like Lycoat and Ludiflash in different concentrations with Gelatin, Poly vinyl alcohol as a film forming agents. The prepared formulations of films were evaluated for film thickness measurement, folding endurance study, in-vitro disintegration time, in-vitro drug release pattern (in pH 6.8 phosphate buffer). Drug content, and drug-polymers interaction study (IR spectroscopy). Among all formulations, the formulation (F12) prepared by 450mg of Lycoat show good drug release (99.37±1.45%).

FORMULATION AND INVITRO EVALUATION OF ROFLUMILAST ORALLY DISINTEGRATING TABLET

V Naga Keerthi Priya — 2024-11-22

An Orally disintegrating tablet disperses readily in saliva and the drug is available in solution or suspension form for the immediate absorption and resulting in rapid onset of action. In the present research work Roflumilast Oral disintegrating tablet were prepared by Direct Compression Technique using varying concentrations of Croscarmellose Sodium, Crospovidone and Ludiflash as super disintegrants. The formulations prepared were evaluated for precompression & post compression parameters. Form the drug excipient compatibility studies we observe that there are no interactions between the pure drug (Roflumilast) and optimized formulation (Roflumilast+ excipients) which indicates there are no physical changes. Post compression parameters was found to be within the limits. Among the formulation prepared the tablet containing 2.5 mg concentration of Ludiflash shows 99.85±1.46% of the drug release within 30 min & follows first order kinetics. The overall result indicated that the formulation F12 containing Ludiflash is better and fulfilling of the needs of the Orally disintegrating tablet.

FORMULATION AND IN VITRO EVALUATION OF GLICLAZIDE CONTAINING NIOSOMES

Dr. Nansri saha — 2024-12-19

In this study niosomal drug delivery system was developed using non-ionic surfactant incorporating Gliclazide by Thin film hydration technique. The prepared niosomal vesicles were quite stable. The formulation was subjected to Entrapment efficiency, Scanning electron microscopy, Invitro release, and Zeta potential analysis. From the results of experimental investigation, we concluded that, formulation F13 containing drug with 300:200 μmol (surfactant:cholesterol) ratio was showing higher percentage entrapment with desired sustained release of Gliclazide. Hence formulation F13 was considered as optimized formulation. Invitro release from optimized Gliclazide niosomal formulation (F13) showed extended release for 24 hours. SEM image revealed the vesicles are exist spherical shape and uniform in size. Scanning electron micrograph shows there is no aggregation between the particles. This confirmed the presence of negative charge inducing agent in formulation. The formulation was checked for sterility as per I.P specification. The optimized formulation passes the sterility test. Stability study was carried out for the period of three months at various storage conditions. The results showed that the formulation remains stable at 4°c. The optimized formulation was found to follow zero order release pattern which was revealed by the linearity shown from the plot of Time Vs cumulative percentage drug release. From the drug release kinetic studies, we concluded that the drug was released from niosome by a zero order diffusion controlled mechanism.

PREPARATION AND EVALUATION OF SAFINAMIDE ORAL THIN FILMS

K.Latha Sri — 2024-11-20

A fast-dissolving medicine delivery system provides a solution for people who experience trouble swallowing pills or capsules. This research aims to generate oral thin films of Safinamide via the solvent casting process. Oral thin films were made utilizing several super disintegrants, such as lycoat and crospovidone, in varying ratios alongside gelatin and polyvinyl alcohol as film-forming agents. The formulated films were assessed for film thickness, folding endurance, in-vitro disintegration time, and in-vitro drug release profile in pH 6.8 phosphate buffer. Investigation of drug content and drug-polymer interactions using infrared spectroscopy. Among all formulations, formulation F12, made with 450 mg of crospovidone, exhibited favorable drug release (99.34±1.25%).

FORMULATION AND IN VITRO EVALUATION OF ROFLUMILAST PULSATILE DRUG DELIVERY

K. Neelima Devi, — 2024-12-05

The purpose of the present study was to design and evaluate an Oral, site specific, Pulsatile drug delivery system containing Roflumilast as a model drug, which can be time dependent manner, to modulate the drug level in synchrony is a member of the drug class known as statins It is used for lowering cholesterol based on chrono pharmaceutical considerations. The basic design consists of an insoluble hard gelatin capsule body, filled with powder blend and sealed with a hydrogel plug. The powder blend containing Roflumilast, Crospovidone, Lycoat, Croscarmellose sodium, MCC and talc was prepared and evaluated for flow properties and FTIR studies. From the obtained results, F12 powder blend formulation was selected for further fabrication of pulsatile capsules. Hydrogel plug was formulated in a lone and in combination of hydrophobic polymer like lactose with hydrophilic polymers like HPMC K15M in 1:1, 2:1, and 1:2 ratios to maintain a suitable lag period and it was found that the drug release was controlled by the proportion of polymers used. The prepared formulations were evaluated for drug content, weight variation and In vitro release studies. FTIR studies confirmed that there was no interaction between drug and polymers and In vitro release studies of pulsatile device revealed that increasing hydrophilic polymer content resulted in delayed release of Roflumilast from the pulsincap after a predetermined lag time of 6hrs. Based on in vitro studies performed, PC4F12 was found to be optimized formulation.

PREPARATION AND EVALUATION OF LESINURAD NANOSPONGES BY USING SOLVENT EVAPORATION METHOD

Dr. D.Nirmala — 2024-12-05

In this study Lesinurad Nanosponges were prepared by the solvent evaporation technique. The Nanosponges formulations were prepared by solvent evaporation method employing HPMC K4, Carbopol 934, Sodium Alginate rate retarding polymers using PVA as a co polymer. The compatibility of the drug with formulation components was established by Fourier Transform Infra-Red (FTIR) spectroscopy. The surface morphology, percentage yield, and drug entrapment efficiency of Nanosponges were examined. Shape and surface morphology of the Nano sponges were examined using scanning electron microscopy. Scanning electron microscopy revealed the porous, spherical nature of the Nanosponges. SEM photographs revealed the spherical nature of the Nano sponges in all variations; however, at higher ratios, drug crystals were observed on the nano sponge surface. Increase in the drug/polymer ratio which is in increasing order due to the increase in the concentration of polymer but after certain concentration it was observed that as the ratio of drug to polymer was increased, the particle size decreased. The particle size was found in the range of 500 to 680 nm. The entrapment efficiency of different formulations was found in the range of 57.16±1.35% to 78.12±1.33%. The in vitro release studies revealed that the formulation with higher concentration of penetration enhancer showed greater drug release.

FABRICATION AND EVALUATION OF SUSTAINED RELEASE TABLETS OF GLIPIZIDE

Dr. Nansri saha — 2024-12-20

The aim of this investigation is to style oral doubly a daily sustained unleash matrix tablets of Glipizide 10mg, used for the treatment of anti-diabetic drug from the antidiabetic drug category which might unharness the drug for ten hours. The tablets were ready by the Wet granulation technique mistreatment variable concentrations of sustained unharness polymers HPMC, Eudragit. The compatibility of the polymers was dominated out by FT-IR studies and located to be compatible. Total nine formulations were ready. The Glipizide powder and also the powder- blends of tablets were evaluated for their physical properties like angle of repose, bulk density and sponginess index and located to be smart and satisfactory. The manufactured tablets were evaluated for in method and finished product internal control tests as well as look, dimensions, weight variation, hardness, friability, drug content, and in vitro drug unleash. The dissolution medium used was hydrogen ion concentration half dozen.8. phosphate buffer. All formulations showed acceptable pharmaco-technical properties and complied with in-house specifications for tested parameters. The results of dissolution studies indicated all formulations free up to 10hours and formulation containing HPMC: F3 was the foremost successful formulation with 99.38% drug unharness at the tip of ten hours.

ADVANCEMENTS IN THE TREATMENT OF LIVER DISORDERS USING RESEALED ERYTHROCYTES

Sincy Sebastian — 2024-11-20

Red Blood Cells (RBCs) have distinct qualities including biocompatibility, biodegradability and the ability to release drugs selectively are becoming a viable drug delivery platform these days. The reversible opening of erythrocyte membranes made feasible by recent developments in nanopore technology permits efficient loading and encapsulation of therapeutic drugs. This strategy has the potential to transform both therapeutic and diagnostic applications to be flexible and targeted drug administration. Since resealed erythrocytes can accurately deliver medications while minimizing side effects, they show great potential in both passive and active targeted applications. Erythrocytes also can flex through capillaries and their biconcave form improves their effectiveness as drug transporters. Numerous techniques have been developed for encapsulating pharmaceuticals with erythrocytes, such as electro-encapsulation, hypotonic dilution, and hypotonic haemolysis. Each of these approaches has unique benefits with controlled release and drug loading efficiency. The use of erythrocytes in drug delivery has significant advantages over other factors, such as potential alterations to erythrocyte physiology and the reticuloendothelial system (RES) rapid clearance. In addition, Resealed erythrocytes have demonstrated exceptional potential in delivering antineoplastic medicines, targeting hepatic tumours, and providing enhanced pharmacokinetics in treating liver problems. These carriers may become widely used in therapeutic settings, especially for the facilitated delivery of hormones, steroids, and biopharmaceuticals. The future prospects of erythrocyte-based drug delivery systems as an innovative and attainable strategy in modern medicine are highlighted in this paper.

ROLE OF NANOPARTICLES IN THE TREATMENT OF CANCER: A REVIEW

Rama Devi Korni — 2024-11-20

One of the wide variety of diseases known as cancer is characterized by the unchecked growth of abnormal cells that can enter, destroy, and spread throughout healthy human tissue. An unusual lump, unusual bleeding, chronic cough or breathing difficulties, and weight changes, including unintentional gain or loss, are some of the main signs and symptoms of cancer. Currently, traditional cancer treatments are confined to surgery, radiation, immuno, targeted, and chemotherapy, all of which have the potential to be harmful. However, these conventional anticancer treatments, are challenged by drug resistance, severity, and side effects. To combat this, nanotechnology has been the subject of much research and application in the treatment of cancer. This is because nanotechnology possesses inherent anti-cancer properties owing to its antioxidant action, which also inhibits the formation of tumors. When it comes to treating cancer, nanoparticle-based drug delivery offers several benefits over traditional drug delivery, such as improved stability and biocompatibility, higher permeability and retention effect, and precise targeting. Many anti-cancer drugs, such as 5-fluorouracil, methotrexate, Doxil (doxorubicin), and Abraxane (paclitaxel), have been effectively manufactured using nanomaterials. This study summarizes current developments in the field of cancer treatment and addresses the many kinds of nanoparticles, their benefits, and their targeting mechanisms.

STUDY OF THE FREE RADICAL SCAVENGING ACTIVITY OF EUPHORBIA HIRTA

NADIR EL Mostafa — 2024-12-05

The analysis of the phytochemical composition of Euphorbia hirta identified a range of compounds, including saponins, polyphenols, flavonoids, tannins, terpenoids, coumarins, and cardiac glycosides. Quantitative assessments showed that the methanolic extract from the roots is particularly high in phenolic compounds, measuring 128.45 ± 5.1 μg GAE / mg of extract. In contrast, the methanol extract from the stems had the highest concentration of flavonoids, at 36.11 ± 0.45 μg QE / mg of extract. The antioxidant capacity of the polar extracts was assessed using the DPPHº method, revealing that the root methanol extract exhibited significant antioxidant activity, with an IC50 value of 07.04 ± 0.14 μg / ml. Furthermore, a correlation was observed between the levels of polyphenols and the presence of phenolic compounds.