International Journal of Pharmacy Research & Technology (IJPRT)

Formulation and evaluation of osmotic tablets of Ranolazine

A. VYSHNAVI, V. ANJANEYULU, G.VIJAY KUMAR, G.VIJAY KUMAR — Tue, 21 Mar 2023 00:00:00 +0300

Ranolazine is a clinically effective antianginal agent that has been used as the sodium- dependent calcium ion influx inhibitor and inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle. Osmotic tablets of ranolazine were prepared by using polymers like HPMC K4M, lactose, povidone K-30, carbopol. The effect of the storage at high temperatures at 40°C, 50°C and 60°C for a period of 3 months on the chemical stability of the selected tablets and prediction of the shelf life was also assessed. Nine formulations were formulated. Pre-compression parameters such as Angle of repose, bulk density, Carr’s index, Haunser ratio were evaluated. The purpose of this work was to formulate a solid dosage form for Ranolazine using the principles of osmosis which will bring down its dosing frequency to once a day and at the same time produce a zero-order release system.

Formulation and Evaluation of Fravotriptan Transdermal Patches for the Treatment of Migraine

S. VAGDEVI, KAMERE KISHORE, DR. VIJAY KUMAR GAMPA — Tue, 21 Mar 2023 00:00:00 +0300

Transdermal patches deliver the drug through the skin in a controlled and predetermined manner in order to increase the therapeutic efficacy of drug. Fravotriptan a 2nd generation triptan that has a favorable tolerability profile and patients have reported greater satisfaction. The aim of the present work was to formulate and evaluate transdermal patches of Fravotriptan. For the current study, the transdermal patch containing drug with different ratios of polymeric combinations and varying plasticizer concentration were prepared. The patch was fabricated by solvent casting method. The casting solvents and plasticizers used were ethanol and propylene glycol respectively. The polymers used were HPMC, PVP and EC. The fabricated patches were evaluated for its physicochemical study. From the studies it concluded that F5 (EC and HPMC of 1:4 ratio and plasticizer 2 ml) whose thickness 0.124 mm, weight variation 110 mg, folding endurance 328 times, percentage moisture absorption of 5%, tensile strength of 0.78 kg/cm2 , drug content of 90.42 % and in vitro drug release of 96.3 % may be selected as the optimized formulation. The released kinetics of the optimized formulation follows first order. It can be concluded that it is possible to fabricate a transdermal delivery of Fravotriptan for treatment migraine where the patient acceptance and tolerability profile is high.

Development and characterization of Emtricitabine loaded Nanoparticles

BASAKONDA VENU, G. VIJAY KUMAR — Tue, 21 Mar 2023 00:00:00 +0300

The present study revealed that ionic gelation technique followed by sonication can be used as an effective tool for preparation of Capecitabine nanoparticles. The main is to delay the release of Capecitabine so that the dosing frequency can be reduced by which we may decrease the side effects and improve the patient compliance. Investigation of the preparation, characterization and in vitro delivery of the Capecitabine nanoparticles was carried out. The different formulations of with different concentration of drug-polymer and surfactant were examined and finalized. Encapsulation efficiency of nanoparticles ranged between 68%-81%. The prepared particles showed good drug- loading capacity. The in vitro release studies showed that after the initial burst, all of the drug-loaded batches provided a continuous and slow release of the drug. . Formulation (F-2) showed the highest encapsulation efficiency i.e., 81%. It was found that as the concentration of chitosan increased, the percentage of encapsulation efficiency was also increased.

Design Development and Characterization of Clotrimazole Nano Sponge Gel

SRI CHARAN, K. KISHORE, G. VIJAY KUMAR — Tue, 21 Mar 2023 00:00:00 +0300

Objectives: Nanosponge is a new concept for the drug delivery system. In the present research work, an attempt was made to develop nanosponge based topical hydrogel containing Clotrimazole. Nanosponges are mainly used to provide the sustained release and thereby reduce the side effects caused by conventional dosage form. Methods: Nanosponges were prepared using emulsion solvent diffusion method by using ethyl cellulose and eudragit S 100 in different concentrations. The prepared nanosponges were evaluated for preformulation parameters. The nanosponges formulation of all batches were evaluated for production yield, entrapment efficiency. Optimized formulation was evaluated for SEM analysis and incorporated into a gel base. The nanosponges containing gel was evaluated for pH determination, spreadability, swelling studies, viscosity determination, and in vitro diffusion study using franz diffusion cell for 10 hrs. Results and Discussion: The results of FTIR analysis showed that there is no physical and chemical interaction between drug and other excipients. F2, F5 are considered to be the optimized nanosponge formulation. G1 was considered to be the best formulation. The data from the in vitro release study were fitted to various mathematical models. The results of mathematical model of fitting data obtained indicated the best fit in all cases. Stability study for 1 months at various condition shows G1 has good stability. Conclusion: The study indicates that the rate of drug release can be improved by incorporating drug into the nanosponges and thus it can improve the targeting of the drug at the specific site and thereby reduce systemic toxicity.

Design and characterization of Methotrextate Mucoadhesive Microspheres

BANSALA NEHA, DR.VENU MADHAV KATLA — Tue, 21 Mar 2023 00:00:00 +0300

Present investigation was to formulate and evaluate mucoadhesive microspheres of Methotrexate using chitosan as a mucoadhesive polymer, prepared by simple emulsification phase separation technique using glutaraldehyde as a crosslinking agent. Nine preliminary trial formulations of mucoadhesive microspheres were prepared using different volume (20 mL to 60 mL) of glutaraldehyde (25 % v/v aqueous solution) as crosslinking agent and different crosslinking time of 1 to 3 hr. Polymer to drug ratio was kept constant (5:1).All the nine formulations were subjected for evaluation of drug content and drug entrapment efficiency, particle size, percentage swelling index, percentage mucoadhesion, in vitro drug release study. From these nine preliminary trial formulations F4, F5 and F6 were selected as optimized formulations based on percentage mucoadhesion, sphericity of microspheres, swelling index and in vitro drug release. The drug polymer compatibility studies were carried out using Fourier transform infrared spectroscopy. The morphology of microspheres were characterised by scanning electron microscopy. The optimized formulation were spherical in shape and free flowing in nature with 72.5 %,70.1 % and 66.2 % mucoadhesion after 1 hour and optimum drug entrapment efficiency of 62.08 %, 69.78 % and 73.26 % with the slow release of 93.57 % , 86.27 % and 78.29 % up to 12 hours. From above three optimised formulations F5 was selected as best formulation based on mucoadhesion, drug content and in vitro drug release. As the concentration of glutaraldehyde increased, the mucoadheasiveness decreases showing more crosslinking between drug and polymer.

Formulation and Evaluation of Buccal Patches of Timolol Maleate

VELPOOR DIVYA, G.S. VALLUR, G.VIJAY KUMAR — Tue, 21 Mar 2023 00:00:00 +0300

The present investigation is concerned with the formulation and development of controlled release mucoadhesive buccal patch of Timolol maleate using natural and synthetic polymers. Timolol maleate is a nonselective beta-adrenergic blocker, and having short biological half-life, approximate 4.1 h, and low oral bioavailability. Therefore in order to control the release and increase the residence time these formulations are carried out. Natural polymer such as Chitosan and Synthetic polymers such as HPMC K15M and Eudragit RL100 were used to formulate the buccal patches. Various grades of Tween are used to increase the permeation capacity of the patch. All the formulations were evaluated for Weight Uniformity, Thickness, Folding Endurance, Swelling Index, Drug Content Uniformity, Tensile Strength and In vitro Drug Release. From all the prepared formulations, F6 showed good drug release characteristic. Drug release from the patches follows desire controlled release phenomenon as needed in buccoadhesive drug delivery.

Design And Evaluation of Topical Gel Containing Solid-Lipid Nanoparticles Loaded with Luliconazole

JHANSI YALLAVULA, KIRANMAI MANDAVA, VENU MADHAV — Tue, 21 Mar 2023 00:00:00 +0300

New topical pharmaceutical options are critically needed to obviate fungal infections. Luliconazole is a potent antifungal drug for the treatment of fungal infection. Due to bioavailability barriers of luliconazole, the current study is associated to develop an optimized topical luliconazole solid lipid nanoparticles (SLN) gel formulation against tropical fungal infection with prolonged therapeutic potential. Luliconazole loaded SLN were prepared through the solvent diffusion method using stearic acid & poloxamer 188 and optimized as per their entrapment efficacy. Thereafter, the optimized SLN wes subjected to physicochemical evaluation, followed by the preparation of different gel formulation. The physicochemical parameters of the optimized gel formulation (G3) were evaluated. Further anti-fungal activity of the G3 was determined against the growth of Candida albicans by TLC-Bioautography assay. The results reveal that SLN F6 shows a significant entrapment with 92.13%±0.975 entrapment efficacy. In particle size, size distribution and zeta potential analysis, SLN exhibit a mean particle diameter of ~344.3 nm, PDI of 0.168, intercept value 0.98 and zeta potential ~18.8 mV. The G3 shows a higher entrapment with 91.39%±0.187 entrapment efficacy and in-vitro drug release profile of the G3 with 1.5 % carbopol 934 w/v shown a sustained release profile with 79.57%±0.213 desolvation rate even after 24 hrs. The anti-fungal activity of SLN G3 gel showed a strong zone of inhibition of the growth of C. albicans. Hence, the study concludes that luliconazole loaded SLN G3 gel formulation containing 1.5% w/v carbopol 934 is suitable for topical application and having strong anti-fungal activity.

Forulation And Evaluation of Colon Specific Drug Delivery System of Celecoxib

RUPA RANI, V. ANJANEYULU, G.VIJAY KUMAR — Tue, 21 Mar 2023 00:00:00 +0300

In the present investigation, an attempt was made to formulate the time and pH dependent drug delivery system, reduce the frequency of dose administeration, and prevent ulcerative colitis by developing sustained delayed release tablets using a combination of Eudragit S-100 and L-100 as enteric coating. The core tablets of Celecoxib were prepared using the direct compresion method. The aim of the present study is to develop colon specific drug delivery of Celecoxib sustained release enteric coated tablet for ulcerative colitis using HPMC K-4M as a semisynthetic polymer. The impact of polymer concentration and superdisintegrant concentration was also studied. In-vitro drug release research was performed on the enteric coated Celecoxib tablet using simulated gastric fluid (0.1N HCl) for 2 hours, simulated intestinal fluid (pH 7.4) for 3 hours, and the simulated colonic fluid (pH 6.8) for 7 hours as a dissolution fluid. The study showed that the coating had a significant impact on the lag time before medication release. In the treatment of colonic illness and the oral administration of medications that are unstable and vulnerable to enzymatic degradation in the upper GI tract, colon drug delivery is advantageous. The results also showed that a mixture of Eudragit S-100 and L-100 may be used to coat tablets for medication delivery to the colon.

Formulation and Evaluation of Poorly soluble drug Josamycin by Solid Dispersion

SAGGIDI KAVYA, G. RAMESH, G.VIJAY KUMAR — Tue, 21 Mar 2023 00:00:00 +0300

The objective of the present work is to mask the intensely bitter taste of Josamycin and to formulate an FDT of the taste-masked drug by incorporation of Excipients in the tablets. Method of Josamycin was prepared by solvent evaporation method using methanol as solvent for pH-sensitive polymer: act as the encapsulating medium. The Mixture of Josamycin with PEG 6000 indicates highest increase in solubility with 3.7-folds Josamycin and PEG 6000 (1:2SD) were selected as optimized combinations for Josamycin. The optimized combinations was formulated into Fast dissolving tablet. The optimized combinations were subjected to FT-IR and while dissolution, and accelerated stability studies were performed on their formulations. The physical properties were evaluated with regard to yield, drug content, flow properties, particle size, in vitro drug release and taste. The average size of microspheres was found to be satisfactory in terms of the size and size distribution. The FDTs prepared by direct compression method and evaluated for hardness, thickness, weight variation, friability, disintegration time, drug content, wetting time, in vitro disintegration, in vitro drug release and stability. Result and discussion simulated salivary fluid (pH 6.8) and sufficient flow properties was shown in the drug: polymer ratio.

Solubility Enhancement of Nateglinide by Solid Dispersion and Their Characterization

GOUNIKADI SAI PRAVALLIKA, K. RAMESH, G.VIJAY KUMAR — Tue, 21 Mar 2023 00:00:00 +0300

The aim of the present work is to investigate the possibility of obtaining immediate release tablet of Nateglinide with improved dissolution using Solid dispersion technique. The solubility and dissolution rate of Nateglinide can be enhanced by formulating SDs of Nateglinide with PEG 6000.The solubilization effect of PEG 6000, reduction of particle aggregation of the drug, formation of microcrystalline or amorphous drug, increased wetability and dispersibility, and alteration of the surface properties of the drug particles might be responsible for the enhanced solubility and dissolution rate of Nateglinide from its SD and to some extent in PMs. No endothermic peak of Nateglinide was present in of SDs with PEG 6000 suggesting the absence of crystalline Nateglinide. From FTIR spectroscopy, it was concluded that there was no well defined chemical interaction between Nateglinide and PEG 6000 in SDs and in PMs, as no important new peaks could be observed. The identical composition of Superdisintegrants showed that a substantial shorter time require for disintegration can be obtained and immediate release tablet were prepared. The Nateglinide immediate release tablet (F2) showed 78.72% drug release within first 5 min. and 99.50% drug release with in 30 min. The results showed that the formulation satisfied the objective of fast disintegration, dissolution, % friability, hardness, wetting time, water absorption ratio, ease of administration and safety. Success of the present study recommends a detailed investigation in to in-vivo studies for its effective use in clinical practice.

Formulation Optimization And Evaluation Of Evaluation Of Transdermal Drug Delivery System Of Felodipine

PRAVEEN ENDHARAPU, SOMNATH DE, VENU MADHAV KATLA — Tue, 21 Mar 2023 00:00:00 +0300

Felodipine, a BCS class II calcium channel blocker, is utilized in the administration of hypertension and angina pectoris. Because of the unfortunate dissolvability and low bioavailability of the medication, there is a need to plan an elective course to accomplish a consistent plasma convergence of felodipine for its greatest remedial utility and can be accomplished by transdermal route.In this review, framework type transdermal patches were arranged utilizing various blends of hydrophilic polymer, to be specific, polyvinylpyrrolidone (PVP) and hydrophobic polymer, in particular, ethyl cellulose (EC) by dissolvable dissipation procedure and were oppressed for characterization.The Fourier change infrared examinations affirmed the similarity among medication and polymers. The patches F1 to F7exhibited uniform weight going from 153.3mg to 242.6mg And thickness of F1 to F7 are going from 0.133 to 0.22mm. Among the different clusters, the consistency weight and thickness shows that the polymeric arrangement of the medication is all around scattered in the patches. Every one of the details (F1 to F7) showed genuinely uniform medication content going from 95.77% to 98.67% individually. it is obviously demonstrated that the Felodipine transdermal patches containing Eudragit RS 100 in the proportion of 1:2 (F6) was the best detailing among the pre-arranged patches.

The objective of the work was to formulate and evaluate solid lipid nanoparticles loaded with clozapine for use in the treatment of schizophrenia. Solid Lipid Nanoparticles was prepared by precipitation method using soya lecithin, sodium glycolate. The dr

MEGHANA ROWTHU, VENU MADHAV KATLA — Tue, 21 Mar 2023 00:00:00 +0300

The objective of the work was to formulate and evaluate solid lipid nanoparticles loaded with clozapine for use in the treatment of schizophrenia. Solid Lipid Nanoparticles was prepared by precipitation method using soya lecithin, sodium glycolate. The drug-polymer incompatibility was ruled out by FTIR studies. Evaluation studies like drug content, entrapment efficiency, particle size distribution, zeta potential and in-vitro drug release, for formulation was performed. From the FTIR studies, the drug-polymers compatibility was confirmed, that, the polymer did not interfere with the drug used. Nanoparticles formulations were found to be in solid dispersion form. The entrapment efficiency of the formulation varied from 20.03-52.30 %. The zeta potential was found to be in range of to -4.42 mv to -74.6 mv. The most ideal formulation was F4 since it showed good In-vitro drug release of 94.79 % release at the end of 12 hours. From this study it could be concluded that the formulated solid lipid nanoparticles of clozapine showed good and effective release.

Formulation And Invitro Evaluation Of Nlc Loaded (Transferosomal) Gel Drug Nabumetone

B.RAVINDRA BABU, V. SWAPNA, B.RASAGNA REDDY — Tue, 21 Mar 2023 00:00:00 +0300

The present research work was designed to prepare Nabumetone -loaded nano lipid carriers (NLs) for ocular delivery. NLs were prepared by the emulsification–homogenization method and further optimized by the Box Behnken design. AM-NLs were optimized using the independent constraints of homogenization speed (A), surfactant concentration (B), and lipid concentration (C) to obtain optimal NLs (AM-NLop). The selected AMNLop was further converted into a sol-gel system using a mucoadhesive polymer blend of sodium alginate and hydroxyl propyl methyl cellulose (AM-NLopIG). The sol-gel system was further characterized for drug release, permeation, hydration, irritation, histopathology, and antibacterial activity.

Formulation And Evaluation Of Gabapentin Nano Gastroenteric Drug Delivery System

B.RAVINDRA BABU, V. SWAPNA, BHAVANI — Tue, 21 Mar 2023 00:00:00 +0300

Background: Gabapentin is an anticonvulsant drug prescribed to treat partial seizures and neuropathic pain. Nisomes as a type of lipid based drug carriers can improve the pharmacokinetic properties of therapeutic agents. In this study, a niosomal formulation was developed for gabapentin, and then, the cytotoxicity effect of the best niosomal formulation was evaluated on normal cells and colon cancer cell lines. Conclusion: The best developed niosomal formulation of gabapentin exhibited good stablity on storage and had a slow and prolonged release of Gabapentin. This niosomal formulation of gabapentin showed cytotoxic effects on colon cancer cells, without significant toxic effect on normal fibroblast cells.

Design And Development Of Nanotechnology Based Oral Formulations Of Tolbutamide Using Biodegradable Polymer

B.RAVINDRA BABU, V. SWAPNA, SRAVYA — Tue, 21 Mar 2023 00:00:00 +0300

The present study concerns the development, characterization, and optimization of nanoparticulate oral formulations of Tolbutamide using poly (ԑ-caprolactone) which is a biodegradable polymer. Emulsion Solvent Evaporation technique was used for preparation of drug-loaded polymeric nanoparticles. This research was carried out to improve the therapeutic efficacy of tolbutamide by increasing its bioavailability through size reduction and to achieve the sustained release of drugs by preparing polymeric nanoparticles. The results of FTIR and DSC analysis indicated that there was no significant interaction between drug and excipients. The prepared drug-loaded Poly (ԑ-caprolactone) nanoparticles were characterized for their surface characteristics via morphology, particle size, stability by zeta potential and drug loading efficiency. The prepared nanoparticles were found to in nanosized range with spherical morphology and stable. The free drug particles can be seen on the polymeric surface which attributes to burst effect and immediate onset of action. The sustained release of drugs through polymeric matrix is evident from drug release studies. This investigation demonstrated the effective application of enhanced bioavailability through the sustained drug release profile of tolbutamide loaded nano-carrier system.

Liquid Solid Compaction Technique : Advances The Stability, Dissolving Rate And Oral Bioavailability Of Poorly Soluble Drug – Pioglitazone

V. SWAPNA, B.RAVINDRA BABU, BHASKAR — Tue, 21 Mar 2023 00:00:00 +0300

The aim of present study is to enhance the dissolution of poorly water soluble drug of Pioglitazone HCl by liquisolid compact technique. Liquid solid compact were prepared using PEG-400 as non-volatile solvent, Microcrystalline cellulose as carrier and cross povidone as superdisintegrant.The compatibility of excipients and drug was confirmed by FT-IR studies. The dissolution studies for prepared liquid solid tablet were distinctly higher as compared to directly compressed tablets which show significance increased in wetting properties and surface area of drug available for dissolution. The optimized formulation of liquid solid pioglitazone tablet shows higher drug release when compared to marketed formulation. The mechanism of drug release studied for best formulations where fitted in accordance with higuchi model and korsemeyer peppas model it is evident that a linear relationship was obtained showing that is an apparent first order process.

Formulation And Evaluation of Acyclovir Hydrogel For Topical Delivery

PURNIMA SHUKLA, DR.S.NAYAK, GARIMA INDURKHYA — Sat, 29 Jul 2023 00:00:00 +0300

Acyclovir has low bioavailability mainly due to low solubility. This study aimed to formulate an optimized acyclovir (ACV) nanoemulsion gel for the slow, variable and incomplete oral drug absorption in patient suffering from herpes simplex viral infection. The dispersion solubility of acyclovir was studied in various oils, surfactants and co-surfactants and by constructing pseudo phase ternary diagram nanoemulsion area was identified. The optimized formulations of nanoemulsions were subjected to thermodynamic stability tests. After stability study, stable formulation was characterized for droplet size, pH determination, centrifugation, % drug content in nanoemulsion, Zeta Potential and Vesicle size measurement and than nanoemulsion gel were prepared and characterized for spreadability, measurement of viscosity, drug content, In-vitro diffusion, in-vitro release data. Span 40 was selected as surfactant, PEG 400 as co surfactant and castor oil as oil component based on solubility study. The in vitro drug release from acyclovir nanoemulsion gel was found to be considerably higher in comparison to that of the pure drug. The in-vitro diffusion of nanoemulsion gel was significantly good. Based on this study, it can be concluded the solubility and permeability of acyclovir can be increased by formulating into nanoemulsion gel.

A Study on The Interrelation of Anxiety and Depression with Diabetes Mellitus

RAZIYA BEGUM SHAIK, NORI KODANDA RAM — Sat, 29 Jul 2023 00:00:00 +0300

The present study aimed to determine the association between anxiety and depression in patients with type 2 diabetes mellitus. All patients with diabetes (182 patients) whose data were recorded in Narasaraopeta and Palanadu district hospitals. Data such as socio-demographic information and depression and anxiety assessment tools. The age range of 40-50 years was found to be more at 36.81%, 56.59% women and 55.49% married, 38.45% had a degree, 47.25% are unemployed, 64.84% are from the city, and 52.20% and 67.58% are non-drinkers and non-smokers; 69.23% have no history of diabetes and 81.87% have no history of the disease, 65.93% were found to be type 2 diabetics, Among 43.41% with diabetes ≥ 10 years, 41.76% were under insulin oral hypoglycemic agents, 43.41% have 200-300 mg/dL, 53.30% have 5-10% hbA1c; approximately 40.11% for depression and 34.07% for anxiety. Most hospitalized patients with diabetes developed moderate/severe anxiety or depression, or both, during hospitalization. Screening for anxiety and depression in high-risk diabetics is therefore recommended with proper supervision.