Sustained Release Dosage Form Research Articles

Sustained release delivery of favipiravir through statistically optimized, chemically cross-linked, pH-sensitive, swellable hydrogel.

In the current work, favipiravir (an antiviral drug) loaded pH-responsive polymeric hydrogels were developed by the free redical polymerization technique. Box-Behnken design method via Design Expert version 11 was employed to furnish the composition of all hydrogel formulations. Here, polyethylene glycol (PEG) has been utilized as a polymer, acrylic acid (AA) as a monomer, and potassium persulfate (KPS) and methylene-bisacrylamide (MBA) as initiator and cross-linker, respectively. All networks were evaluated for in-vitro drug release (%), sol-gel fraction (%), swelling studies (%), porosity (%), percentage entrapment efficiency, and chemical compatibilities. According to findings, the swelling was pH sensitive and was shown to be greatest at a pH of 6.8 (2500%). The optimum gel fraction offered was 97.8%. A sufficient porosity allows the hydrogel to load a substantial amount of favipiravir despite its hydrophobic behavior. Hydrogels exhibited maximum entrapment efficiency of favipiravir upto 98%. The in-vitro release studies of drug-formulated hydrogel revealed that the drug release from hydrogel was between 85 to 110% within 24 h. Drug-release kinetic results showed that the Korsmeyer Peppas model was followed by most of the developed formulations based on the R2 value. In conclusion, the hydrogel-based technology proved to be an excellent option for creating the sustained-release dosage form of the antiviral drug favipiravir.

Compritol®-based solid lipid nanoparticles of desvenlafaxine prepared by ultrasonication-assisted hot-melt encapsulation to modify its release.

Aims: Desvenlafaxine (DES) in conventional dosage forms shows initial burst release after oral administration, leading to exaggeration of its side effects. These side effects can be overcome by a sustained-release dosage form using the chemically inert, low-melting-point lipid Compritol® 888 ATO, as it reduces initial burst release. Materials & methods: The potential of DES-loaded solid lipid nanoparticles (DES-SLNs) synthesized by ultrasonication-assisted hot-melt encapsulation to modify the release of DES was investigated. Results: The entrapment efficiency of DES-SLNs was 65.90% with the in vitro release profile showing a sustained-release behavior achieving 81% cumulative release within 16h without initial burst release. Conclusion: DES-SLNs are a potential carrier for sustained release of water-soluble antidepressant drugs such as DES.

Formulation and Evaluation of Glipizide-loaded Mucoadhesive Microparticle Using Salvia hispanica Seeds Mucilage as Co-polymer

Aims: Chia seed (Salvia hispanica L.) gum is a mucoadhesive, biodegradable polymer with sustained release properties. Objective: The objective of this study was to compare different formulations of glipizide-loaded microparticles using chia seed mucilage and sodium alginate, focusing on sustained release and mucoadhesive properties. Background: The present study aimed to comparatively evaluate various eco-friendly formulations of glipizide-loaded microparticles prepared using chia seed mucilage and sodium alginate. Materials and Methods: Gum was extracted from chia seeds and lyophilized, and preformulation studies were performed according to established protocols. Microparticles were formulated using the ionic gelation method, with sodium alginate as a copolymer and zinc chloride as a cross-linking agent. The prepared microparticles were evaluated using scanning electron microscopy (SEM) for size and particle aggregation, and Fourier Transform infrared spectroscopy (FTIR) for drug-polymer interaction, entrapment efficiency, swelling index, and in vitro drug release. Results: The % yield of chia seed mucilage was 27.35%. The pH of the mucilaginous suspension was 4.67 ± 0.50. The moisture content value was 14.56 % ± 0.50. The values of Carr's index and Hausner's ratio were 22.58 ± 1.89 and 1.38 ± 0.05, respectively. FTIR spectra showed no interaction between pure glipizide and chia seed mucilage, confirming no possible change in glipizide's pharmacology. SEM studies have confirmed the shape of the microparticles to be spherical, with average sizes ranging from 1235.18 ± 8.7 to 1423.25 ± 9.5 µm, and the drug entrapment efficiency ranged from 64.25 ± 2.52 to 81.82 ± 7.56%. The release of glipizide from the microparticles was sustained, and the Higuchi and Korsmeyer-Peppas models were found to be the best-fit kinetic models. Conclusion: The promising copolymer blend of chia seed mucilage and sodium alginate was used for the development of sustained-release dosage forms. A copolymer blend with a ratio of 1:1 produced glipizide-loaded microparticles with sustained release profiles and good mucoadhesive ability, along with a high percentage of drug entrapment efficiency.

Improved Mucoadhesive Properties of Repaglinide-Loaded Nanoparticles: Mathematical Modelling through Machine Learning-Based Approach

This research work aims to develop a modified repaglinide-loaded chitosan-ethyl cellulose nanoparticles (RPG-ECSNPs) as a novel sustained-release dosage form with improved mucoadhesive properties using an emulsification solvent-evaporation technique. The RPG-ECSNPs with different particle sizes were prepared from various polymers containing ethyl cellulose (EC) as the internal phase and chitosan (CS) as the external phase, and the use of surfactants, including Tween 80 and poloxamer 188 as emulsifiers. In vitro drug release, drug loading amount, and entrapment efficiency have been influenced by changes in the concentrations of CS and EC. The mean droplet size and zeta potential of RPG-ECSNPs were 213 ± 8.5 nm and 16.4 ± 2.4 mV, respectively. The optimized formulation's entrapment efficiency was 66 ± 2.3%, and drug loading was 7.9 ± 1.65%. The release profile was significantly higher in PBS (90%) than in diluted hydrochloric acid (30%) during 24 h of the study. The mucoadhesive function of the particles was examined in vitro using part of rat intestines. The highest adhesive % was observed for the chitosan-coated NPs. No adhesive properties were noticed for chitosan-free NPs (P-value > 0.05). This indicated that ECSNPs can be successfully utilized for sustained and controlled drug delivery of RPG through the GIT.

The cytisine-enriched poly(3-hydroxybutyrate) fibers for sustained-release dosage form

The polymeric cytisine-enriched fibers based on poly(3-hydroxybutyrate) were obtained using electrospinning method. The biocompatibility study, advanced thermal analysis and release of cytisine from the poly(3-hydroxybutyrate) fibers were carried out. The nanofibers' morphology was evaluated by scanning electron microscopy. The formation and description of phases during the thermal processes of fibers by the advanced thermal analysis were examined. The new quantitative thermal analysis of polymeric fibers with cytisine phases based on vibrational, solid and liquid heat capacities was presented. The apparent heat capacity of fibers was measured using the standard differential scanning calorimetry. The quantitative analysis allowed for the study of the glass transition and melting/crystallization process. The mobile amorphous fraction, degree of crystallinity and rigid amorphous fraction were determined depending on the thermal history of semicrystalline polymeric fibers. Furthermore, the cytisine dissolution behaviour was studied. It was observed that the kinetic of the release from polymeric nanofiber is delayed than for the marketed product. The immunosafety of the tested polymeric nanofibers with cytisine was confirmed by the Food and Drug Agency Guidance as well as the European Medicines Agency. The polymeric matrix with cytisine seems to be a promising candidate for the prolonged release formulation.

Formulation design and optimization of sustained release tablet dosage form of Diacerein

Diacerein is both an anti-inflammatory drug and an anti-arthritic agent. At present, no sustained release dosage form of Diacerein is commercially available. The aim of the study was to develop an optimized formulation of sustained release tablet dosage form of Diacerein that will be highly patient compliant. A three-level full factorial design was employed to develop nine different formulations of matrix tablets using a combination of Methocel K100M CR and Methocel K4M CR polymer at different ratios. The physical evaluation of both the drug-excipient powder mixtures and tablets of the nine formulations were performed and results were found to be within acceptable ranges for all tests. Dissolution profiles of tablets were obtained and the kinetics of drug release from the matrix tablets were determined by employing various mathematical models. The release data were simulated in Design Expert Software to carry out statistical analysis and the effect of both polymers on release patterns were observed after 1, 4 and 8 h in terms of contour plots and 3D surface plots, which were found to be statistically significant (p < 0.05). Finally, the overlay plot was obtained from which the optimized formulation of Diacerein was determined.

Formulation and Characterization of Montelukast Sodium Mouth Dissolving Film Using Cress Seed Mucilage

There is a rising interest in the development of orodispersible films (ODFs) as an alternative to fast dissolving tablets which is attributed to their faster dissolution rate, higher durability, and better patient compliance. Owing to its rheological and also various functional properties, many researchers tried to discover some of the pharmaceutical applications of L. sativum in the development of various dosage forms, in addition to its therapeutic studies, such as binding, dissolving, gelling and sustained release dosage form. The fast-dissolving oral film of the Montelukast sodium by using Cress seed mucilage (CSM) and HPMC (15cps) is prepared by solvent casting method. The fast-dissolving oral film evaluated for folding endurance, surface pH, in-vitro disintegration time, drug content and in-vitro drug release. The physical appearance and folding endurance properties were found to be reasonably good and electron microscopy shows that films are clear, colorless with smooth surface.The drug content of all the films was in the range suggesting that drug was uniformly dispersed throughout all films. The present study was an attempt to develop and evaluate an oral fast dissolving drug delivery system using cress seed mucilage as a film former.&#x0D; Keywords: Orodispersible film, Montelukast sodium, Cress seed mucilage, HPMC

Review: Therapetic Approach in the Management of Osteoarthritis

Objectives: The goal in designing sustained or controlled delivery systems is to reduce the frequency of dosing or to increase the effectiveness of the drug by localization at the site of action, reducing the dose required, and providing uniform drug delivery. A sustained release system is a type of modified drug delivery system that can be used as an alternative to a conventional drug delivery system.&#x0D; Summary: Osteoarthritis is a generative disease of synovial joints characterized by focal loss of articular hyaline cartilage with the proliferation of new bones and remodelling of joint contour. Risk factors of osteoarthritis are age, female gender, joint alignment, hereditary gene defect, joint injury and obesity.There are various symptoms of osteoarthritis and It diagnose by blood test, joint fluid test and MRI. Osteoarthritis is treated by self-care, medications, therapies, and surgeries. A sustained-release dosage form is a dosage form that maintains the therapeutic blood or tissue levels of the drug by continuous release of medication. Formulation of granules by wet granulation and the granules are evaluated by the pre-compression and post-compression studies.&#x0D; Conclusion: Sustained release tablet optimize drug release for extended time period.It maximized effectiveness, reduced side-effects of drug and cures the disease.&#x0D;

PREPARATION AND EVALUATION OF ONCE-DAILY FLOATING GMO-ALGINATE MICROSPHERES CONTAINING FAMOTIDINE

Objective: In this work, a gastro-retentive floating microsphere delivery system composed of Drug/Glyceryl mono-oleate (GMO) embedded in a Ca-alginate gas-generated matrix was designed to improve the bioavailability of a slightly-soluble model drug Famotidine. Methods: The water/Oil emulsion method was used to prepare Famotidine floatable microspheres, and formulation variables such as Alginate: GMO ratio, gas-generated bicarbonates concentration, and loading drug concentration were investigated. Conventional techniques, including DSC, XRD and FTIR were performed to confirm Famotidine compatibility with GMO and Alginate polymers. Real-Time X-ray Radiography was used for in vivo imaging of Famotidine floatable microspheres using rabbits as an animal model. HPLC spectroscopic technique was used to determine Famotidine plasma concentration after oral administration of Alginate-GMO loaded microspheres. Results: Floating Famotidine Alginate-GMO microspheres (0.75:1:0.25) w/w/w showed a remarkable entrapment efficiency (&gt;98%), good buoyancy (&gt;84) and prolonged in vitro drug release properties (&gt;24 hours). DSC, XRD, and FTIR techniques showed no evidence of interaction between Famotidine and Alginate or GMO. In vivo Imaging of Famotidine floatable microspheres showed that capsules containing Famotidine-Alginate microspheres were not detected after 3 h of administration, while capsules containing Famotidine-GMO-Alginate microspheres can be detected for more than 12 h, indicating superior gastric retention properties. The pharmacokinetic parameters were calculated for Famotidine: GMO-Alginate, and Famotidine: alginate and compared with the plain drug over 24 h period. Famotidine: GMO-Alginate microspheres exhibited controlled and prolonged absorption Tmax of 6.0 vs. 3.0 and 2.0 h; Cmax of 124.9±0.9 vs. 323.7±0.4and 458.6±0.5 ng/ml; AUC0-24 of 2153.025±6.7 vs. 1650.4±1.9 and 1110.725±2.1 ng/ml for Famotidine: alginate and plain drug, respectively, reflecting the increase in the bioavailability of the drug in the floating formulations compared to the free drug. Conclusion: Prolonged gastric retention time and sustained release properties of floating GMO-alginate microsphere suggest that it could provide a valuable sustained release dosage form of slightly-soluble drugs.

Novel Approaches of Polyherbal Matrix Tablet and its Evaluation Parameters

According to WHO, approximately 80 percent of people in developing countries still rely on traditional medicine, which is based primarily on plant and animal species, for primary health care. Because of the toxicity and side effects of allopathic drugs, herbal therapy is becoming more popular. Medicinal plants are crucial in the development of powerful therapeutic agents. Natural products derived from plants, animals, and minerals have long been used to treat human disease Plant medicines are frequently used in combination rather than alone to maximise the benefit of their combined strength. Because of synergism, polyherbalism provides a variety of benefits not found in single herbal formulations. Polymers are the building blocks of a pharmaceutical drug delivery system because they control drug release from the device. Polymers are used to protect drugs from the physiological environment and to extend their release time in order to improve their stability. This review focuses on matrix tablets, which are one of the most practical methods for developing sustained-release dosage forms, as well as the approaches used in their formulation and evaluation. The therapeutic efficacy of a sustained release matrix tablet with improved efficacy can be increased. It also emphasizes the significance of polyherbalism and matrix Tablet.

Eudragit RS/RL을 이용한 고체분산에 의한 티카그렐러 서방형 제형 설계

티카그렐러는 급성관상동맥증후군 환자의 뇌졸중과 심장마비를 예방하는 약물로서 용해도와 생체막 투과성이 낮은 생물약제학적 분류체계 IV에 속하는 약물이다. 이에 생체이용률을 높이기 위해서는 약물가용화 과정이 필수적이다. 이를 위해 친수성이고 pH 비의존적 고분자 Eudragit RL PO, Eudragit RS PO을 사용해 분무건조법으로 습식과립공정을 통해 고체 분산체를 제조하였다. 약물이 무정형으로 고분자 매트릭스에 분산되었는지 X-ray diffractometer, differential scanning calorimetry를 통해 결정성 및 포접을 확인하였고, Fourier transform infrared spectroscopy을 통해 화학적 변화를 확인하였다. 최종적으로, 용출시험을 통해 약물의 방출제어가 잘 이루어졌는지 확인하여, 복용 회수를 줄이고 환자의 복약 순응도를 높인 제형으로 개발 가능함을 확인하였다.

Method of Starch Acetylation and Use of Acetylated Starch as Polymer in Pharmaceutical Formulations

Starch is used as a key polymer in pharmaceutical industries since long back for various purposes such as binder, disintegrating agent, bulking agent, film former and many more. But as per the purpose of dosage forms it’s used get changed. Currently scientists are more focused on controlled and sustained release dosage forms. Since, native starch does not meet up the demand of controlled or sustained release, so there is need of modifying the polymer as per dosage form requirement. Modification of starch can be done by physical, chemical, enzymatic, and genetic method. Among all, the current article is focusing on chemical modification of starch, especially the acetylation. Acetylation of starch can be done using different acetylating agent such as acetic anhydride (AA), and glacial acetic acid etc. and sodium hydroxide (NaOH), pyridine and sulphuric acid etc as a catalyst. The native structure of starch can be less efficient, since its functional properties are less stable to process condition such as high temperature, shear stress and exposure to acidic media, which decreases its use in industrial application. Acetylated starches facilitate higher stability and resistance to retrogradation or crystallization, enhanced granular size, swelling power, and water absorption capacity, which provides good flow and compression properties. It reduces the pasting temperature and solubility. It makes the acetylated starch as a good candidate for customizing the overall performance of native starch, which may be used as the controlled release or sustained release polymer in pharmaceutical dosage form.

Formulation and Evaluation of Sustained Release Solid Dispersed Nifedipine Microcapsules

Conventional drug delivery system for treating the angina and hypertension are not much effective as the drug do not reach the site of action in appropriate amounts. Thus potent and guarded therapy of this angina and hypertension disorder using specific drug delivery system is a challenging task to the pharmaceutical professionals. The study was aimed at increase the solubility of poorly soluble drug nifedipine and formulating it in sustained release dosage form. Solid dispersion of drug was prepared using Poly vinyl pyrrolidone (PVP) as inert hydrophilic carriers by solvent evaporation technique. A 17-fold increase in dissolution rate of nifedipine was observed with solid dispersion prepared with PVP (K30). Sustained release microcapsules of nifedipine were formulated using Eudragit RS 100 as a polymer, acetone as polymer solvent for Eudragit RS100, N-hexane as a non-solvent, liquid paraffin vehicle, with solid dispersion of nifedipine as core by emulsion solvent evaporation method and modified emulsion solvent evaporation method. Microcapsules from all the batches were found to discrete, spherical and free flowing and % entrapment efficiency was found to be in range of 96.01% to 97.87%. All the batches of microcapsules showed sustained release curve in pH 7.4 phosphate buffer up to 12hours with maximum release up to 97.22% after 12hrs was found to be in B2. SEM studies of the microcapsules showed the surface topography states that prepared microspheres were spherical in shape. Shiny and uniform covered surface with polymer. Keywords: Nifedipine, Poly vinyl pyrrolidone, Solid dispersion, Microcapsules, Emulsion solvent evaporation method

A brief overview of sustained released drug delivery system

The most popular and patient-friendly method of drug administration is often thought to be the oral route of administration. Compared to conventional release formulations, advancements in formulation technology, including modified release dosage forms or sustained release oral dosage forms, have been extensively accepted. A sustained release dosage form provides a prolonged release of the drug over an extended period, thereby giving better patient compliance and enhanced bioavailability. Sustain release systems are considered a wiser approach for drugs with short half-lives requiring repeated dosing. Sustained release drug delivery has a range of advantages over conventional dosage forms, including increased patient compliance due to less frequent drug administration, significantly reduced steady state drug level fluctuations, maximum drug utilization, the increased safety margin of potent drugs, lower healthcare costs due to improved therapy, and shorter treatment times. The present review focuses on design, fabrication, and various factors that influence the performance of sustained-release dosage forms.

EVALUATION OF DIACEREIN MICROSPHERE MANUFACTURED BY FLUID BED BOTTOM SPRAY COATING TECHNIQUE AS SUSTAINED RELEASE DRUG DELIVERY FORM

Diacerein (DCN), an anti- inflammatory, anti-osteoarthritic drug having short-acting properties was formulated as microsphere following fluid bed bottom spray coating technique for sustained release drug delivery, where HPMC (6cps) and ethyl cellulose (N7) were used as coating polymers. Assay of DCN microsphere was done following HPLC method. Drug content in microsphere was found to be 147 mg g-1. Drug entrapment efficiency was calculated as 61%. SEM study of microsphere showed that microsphere was spherical in shape and porous in structure. Particle size, size distribution, zeta potential and poly disparity index were studied by dynamic light scattering method. particle size range was found between 396-615nm, zeta potential 10.8-19.6mv and PDI 0.65. In vitro drug release rate from microsphere was studied in different buffers like phosphate (pH 6.8), citrate (pH 6.0) and acidic medium (0.1N HCL). DCN microsphere released about 97% of its drug content in 20 h in phosphate buffer, 57.8% of its drug content in citrate buffer in 20 h and negligible drug release was found in acidic medium. On the contrary, market preparation of diacerein 50 mg capsule (Orcerin, Macleod’s) released 80% of its drug content in 1 h in phosphate and citrate buffer. Pharmacokinetic study of DCN microsphere vis a vis DCN capsule market preparation in plasma level of rabbit showed as Cmax4.02/3.97 mcg ,Tmax4h/ 2.67h, AUC0-t 21.26/17.80 mcg h mL-1, AUC 0-∞ 21.35/19.38 mcg h mL-1, T1/2 1.98/ 2.30 h and Kel 0.35/0.31. Study as mentioned above showed that DCN microsphere manufactured by fluid bed bottom spray coating technique using HPMC (6cps) and ethyl cellulose (N7) as coating polymers exhibited sustained release drug delivery. So it is a useful method for manufacture of sustained release dosage form.

Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility.

A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmental pHs. The best approach is to increase the dissolution rate of the drugs at the different pHs and only then modify its release behavior from the pharmaceutical form. This work aims to demonstrate the ability of properly designed polymeric nanofibers in enhancing the release rate of model drugs with different pH-dependent solubility in the different physiological pHs of the gastrointestinal tract. Polymeric nanofibers loaded with meloxicam and carvedilol were prepared using the electrospinning technique and were then included in properly designed tablet formulations to obtain fast or sustained release dosage forms. The nanofibers and the tablets were characterized for their morphological, physico-chemical and dissolution properties. The tablets are able to deliver the dose according to the expected release behavior, and zero-order, first-order, Higuchi, Korsmeyer–Peppas and Hixon–Crowell kinetics models were used to analyze the prevailing release mechanism of the tablets. This study shows that the electrospun fibers can be advantageously included in oral dosage forms to improve their release performances.

Development and characterisation of methylphenidate hydrochloride loaded nanoparticles

Preparation of Methylphenidate Hydrochloride nanoparticles was the goal of this study, which aimed to minimise the dosage frequency. Polymeric nanoparticles are gaining in popularity due to their inertness, solubility in non-toxic solvents, and ability to be used to create sustained-release dosage forms, among other characteristics. Melphenidate hydrochloride, a diuretic, is used to treat congestive heart failure, edoema, and renal failure among other conditions. Polymeric nanoparticles are one of the most effective platforms for long-term release because of their high stability. To put it another way, because its half-life (2.4 hours for children and 2.1 for adults) is short, methylphenidate hydrochloride is only effective for an extremely short period of time. This study's major focus is on nanoparticles. Eudragit RL 100 can be used as a release retardant. Formulation of Methylphenidate Hydrochloride and Eudragit RL 100 nanoparticles in order to provide long-term activity and hence boost bioavailability. The steady release of Methylphenidate Hydrochloride from nanoparticles increases therapeutic efficacy by maintaining a constant drug plasma concentration. The new formulation of methylphenidate hydrochloride sustained release proved successful in alleviating the problems associated with the old one.

Formulation and evaluation of sustained release tablets of propranolol hydrochloride

The main objective of sustained release drug delivery system is to provide a steady state blood plasma level concentration which is non-toxic and therapeutically active for a longer period of time. Owing its increased patient compliance and prolonged release of action in delivering drugs several benefits can be contemplated in delivering of sustained release dosage form[1]. Among various route of drug delivery Sustained release drug delivery is most widely preferred as it’s less frequency of dosing and controls the release of drugs. Natural polymers are biodegradable and nontoxic in nature with reduced side effects. It is also eco-friendly and safe to be administered as compared to synthetic polymers. The current work was based on preparation of sustained release tablets of Propranolol Hydrochloride using natural polymers like Gum Acacia, Hibiscus Rosasinesis and Microcrystalline cellulose. Presently much attention is being paid for formulation of sustained release tablets that contains matrix system. Direct compression method was used for formulation of sustained release tablets of Propranolol Hydrochloride. The prepared tablets were evaluated for different pre-formulation studies and in vitro dissolution studies were performed using USP-III dissolution apparatus. Dissolution studies of different formulations were evaluated for 24 hours at 370C.

Development of a Novel Methotrexate-Loaded Nanoemulsion for Rheumatoid Arthritis Treatment with Site-Specific Targeting Subcutaneous Delivery.

Rheumatoid arthritis (RA) is a systemic, chronic autoimmune disease that causes disability due to progressive inflammation and destruction of the tissues around the joints. Methotrexate is mainly used to prevent the progression of joint destruction and reduce the deformity. The major challenge in treating RA with methotrexate is the systemic side effects that limit dose escalation. Hence, a novel formulation of a methotrexate-loaded nanoemulsion for subcutaneous administration was developed that aims to deliver methotrexate into the system via the lymph. The methotrexate-loaded nanoemulsion was prepared by using the aqueous-titration method. The prepared nanoemulsion was investigated for particle size, surface charge, surface morphology, entrapment efficiency, DSC (differential scanning colorimetry), drug release, hemocompatibility assay, and cytotoxicity, as well as anti-arthritic and stability studies. The vesicle size, zeta potential, PDI (polydispersity index), and entrapment efficiency of the optimized nanoemulsion were 87.89 ± 2.86 nm, 35.9 ± 0.73 mV, 0.27, and 87 ± 0.25%, respectively. The DSC study showed that the crystalline methotrexate was converted to an amorphous form and the drug was fully incorporated into the vesicles. After 72 h, the optimized nanoemulsion showed a drug release of 96.77 ± 0.63%, indicating a sustained-release dosage form. Cytocompatibility testing by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) assay on macrophage cell lines showed that the nanoemulsion was non-toxic. The formulation showed significant anti-arthritic activity compared to the marketed drug solution. In addition, the nanoemulsion containing methotrexate remained stable for three months when stored at a low temperature. Since the nanoemulsion containing methotrexate has excellent physicochemical properties and lowers systemic side effects by targeted delivery, it is a desirable technology for subcutaneous drug delivery.

Formulation, Development and Characterization of Sustained Release Formulation of Herbal Extracts

Aim: The aim of the present investigation is to design of sustained release dosage form of different extracts that will help in releasing only small quantities of drug over a prolonged period of time. Material and Methods: The different ingredients for formulations are given as in Table 1 below. The measured quantities of drug, HPMC, MCC and NaHCO3 were mixed thoroughly using a mortar and pistil. The granules were punched into tablets using direct compression technique. The blank formulation (or) placebo (HPMC+ MCC+NaHCO3) and polyherbal formulation were also tested using FTIR Spectrometer. The release rate kinetics of the formulations was analyzed and the data obtained were fitted into Zero order, First order, Higuchi model and Kozmeyer Peppas model. Results: The pre-formulation study results obtained on various parameters on granules were found satisfactory. The granules obtained for the batches (F1-F12) were satisfactory. No rat holing, capping or sticking was observed during the flow of granules from the hopper. The maximum weight variation of the tablets was±1.8%, which falls within the acceptable range of±5%, hence the tablets passed the weight variation test. Hardness for tablets of all batches was in the range of 4.92 to 5.35 kg/cm², which falls above the limit of not less than 3.0 kg/cm². The floating lag time ranged from 35 s to 50 s. From the Table 5, it was found that the formulation F11 has the minimum floating lag time of 35 s and maximum total floating time of 15 h with 100.12% drug content. Conclusion: The effect of ingredients in the polyherbal tablet was analyzed, where HPMC contributed as the floating matrix, MCC to increase the bulk density of the tablet and sodium bicarbonate to initiate the dissolution process.