Controlled Release Dosage Forms Research Articles

A Comprehensive Review of Challenges in Oral Drug Delivery Systems and Recent Advancements in Innovative Design Strategies.

The oral route of drug administration is often preferred by patients and healthcare providers due to its convenience, ease of use, non-invasiveness, and patient acceptance. However, traditional oral dosage forms have several limitations, including low bioavailability, limited drug loading capacity, and stability and storage issues, particularly with solutions and suspensions. Over the years, researchers have dedicated considerable effort to developing novel oral drug delivery systems to overcome these limitations. This review discusses various challenges associated with oral drug delivery systems, including biological, pharmaceutical, and physicochemical barriers. It also explores common delivery approaches, such as gastroretentive drug delivery, small intestine drug delivery, and colon-targeting drug delivery systems. Additionally, numerous strategies aimed at improving oral drug delivery efficiency are reviewed, including solid dispersion, absorption enhancers, lipidbased formulations, nanoparticles, polymer-based nanocarriers, liposomal formulations, microencapsulation, and micellar formulations. Furthermore, innovative approaches like orally disintegrating tablets (ODT), orally disintegrating films (ODF), layered tablets, micro particulates, self-nano emulsifying formulations (SNEF), and controlled release dosage forms are explored for their potential in enhancing oral drug delivery efficiency and promoting patients' compliance. Overall, this review highlights significant progress in addressing challenges in the pharmaceutical industry and clinical settings, offering novel approaches for the development of effective oral drug delivery systems.

Modelling nematic liquid crystal in fractal dimensions

In this paper we present a fractal Berreman's model which account for azimuthal surface anchoring of nematic liquid crystals which play a leading role nowadays in biomedical field and pharmaceutical controlled release dosage forms. The model is based on the concept of "product-like fractal measure" in anisotropic media which permits to describe liquid crystals formation in terms of fractal dimensions. It was observed that fractal dimensions affect both the polar azimuthal angle and the Franck excess elastic energy density of the distortion. For fractal dimensions close to unity, our analysis reveals the emergence of fluctuations and large deformations in the dynamical variables of the theory which suggest the presence of non-linear elastic instabilities or emergence of defect structures in liquid crystals. These fluctuations fade away for fractal dimensions much less than unity. We have evaluated the elastic energy per unit of area which is found to depend on the square of the fractal dimension. This leads to a decrease of the saturation voltage which is necessary to reduce the elastic energy of liquid crystals films in order to minimize the elastic energy. This reduction may describe nematic liquid crystals free from deformations, singularities or weak anchoring surfaces.

Mannitol-Coated Hydroxypropyl Methylcellulose as a Directly Compressible Controlled Release Excipient for Moisture-Sensitive Drugs: A Stability Perspective.

Hydroxypropyl methylcellulose (HPMC) is one of the most commonly used hydrophilic polymers in formulations of matrix tablets for controlled release applications. However, HPMC attracts moisture and poses issues with drug stability in formulations containing moisture-sensitive drugs. Herein, the moisture sorption behavior of excipients and drug stability using aspirin as the model drug in matrix tablets were evaluated, using HPMC and the newly developed mannitol-coated HPMC, under accelerated stability conditions (40 °C, 75% relative humidity) with open and closed dishes. Tablets prepared with mannitol-coated HPMC showed a slower drug degradation rate compared to tablets prepared with directly compressible HPMC. Initial moisture content and hygroscopicity were stronger predictors of drug stability compared to water activity when comparing samples without similar moisture content. In the early stage (day 0 to 30), the aspirin degradation rate was similar in both open and closed conditions, as moisture content is the main degradation contributor. In the later stage (day 30 to 90), aspirin degradation was faster under closed conditions than under open conditions, likely due to autocatalytic effects caused by the volatile acidic by-product entrapped in the closed environment. The findings from this study reinforced the importance of judicious excipient selection based on the understanding of excipient-moisture interactions to maximize the chemical stability of moisture-sensitive drugs. Mannitol-coated HPMC is a promising addition to the formulator's toolbox for the formulation of controlled release dosage forms by direct compression.

Formulation and Characterization of Emulgel Lornoxicam Containing Lemon Grass Oil as Penetration Enhancer.

Emulgel dosage form is an advanced form of transdermal drug de-livery. It is a combination of emulsion and gel in a definite ratio. Emulsions are incorporated into the gel with proper mixing. The emulsion present in emulgel can be either oil/water or water/oil, which is thickened by mixing it with a gelling agent. On the basis of the solubility of lornoxicam in various oils, a surfac-tant and a co-surfactant were selected for further research. For the preparation of emulgel, the emulsion was prepared with Smix (surfactant and co-surfactant) in a ratio of 1:2. The prepared emulsion was incorporated into different concentrations of carbapol 934 in a 1:1 ratio to make a homogenous emulgel. The emulgel was inspected visually to see if it had any phase behaviour, spreadabil-ity, or grittiness by applying it to a slide. All formulations were evaluated for pH, physical properties, drug content, spreadability, extrudability, swelling index, viscosity, and centrifu-gation. Franz diffusion cell was used to perform in-vitro release of formulation with the help of egg membrane. Among all formulations, F3 showed 83% release after 6 hours and showed acceptable physical properties like homogeneity, colour, consistency, pH value, spreadability, extrudability, and drug content. Thus, emulgel can be regarded as a more feasible drug delivery system for hy-drophobic drugs (lornoxicam) than the currently marketed formulation. Optimized emulgel formulation consists of a microemulsion of lornoxicam, 1 % of carbopol 934, propylene gly-col, sodium benzoate, lemon grass oil, glycerin, and distilled water. In the in-vitro release studies, pH 7.4 phosphate buffer emulgel formulation (F3) showed 83% after 6 hours. Emulgel was found to be stable under stable conditions. The emulgel of the poorly water-soluble drug (lornoxicam) was formulated. The components and their optimum ratio for the formulation of microemulsion were obtained by solubility studies and droplet size analysis. Thus, microemulsion can be regarded as a more feasible dose delivery system for lornoxicam than the currently marketed tablet, capsule, and injection formulations. Optimized microemulsion of lornoxicam was incorporated into the gel base. Therefore, it may be concluded that emulgel of lornoxicam can be used as a controlled-release dosage form of the drug for local application in rheumatoid arthritis.

HYDROPHILIC MATRIX TABLETS AS ORAL CONTROLLED DRUG DELIVERY SYSTEMS IN 20TH CENTURY: A REVIEW

Matrix systems are easy to formulate compared to other controlled release dosage forms. The manufacture of matrix tablets involves the direct compression of blend of drug, retardant material and additives to form a tablet in which drug is embedded in a matrix core of the retardant. Alternatively, retardant-drug blends may be granulated prior to compression. Of the three classes of retardant material used to formulate matrix tablets, polymers that form hydrophilic matrices are attracting the attention of pharmaceutical technologists. These polymers include Methyl cellulose (MC), Hydroxy ethyl cellulose (HEC), Hydroxy popyl methyl cellulose (HPMC), Sodium carboxy methyl cellulose (NaCMC), carbomers, chitosan, plant gums etc. The hydrophilic matrix-formers alone or in combination with other excipients form gels in situ on coming in contact with biological fluids which control the drug release. The present review gives a detailed account on the factors to be considered in the design of hydrophilic matrix systems, formulation of hydrophilic matrix tablets, in vitro and in vivo evaluation methods and advances in the design of hydrophilic matrix tablets. This review further focuses on the development of oral controlled drug delivery systems using hydrophilic matrix carriers in 20th century.

Formulation and evaluation of sustained release floating tablets of venlafaxine using natural polymers

Over the past three decades, oral controlled-release dosage forms have been developed due to their therapeutic advantages, such as ease of administration, patient compliance, and flexibility in formulation. However, this approach has faced physiological difficulties, such as the inability to contain and position the controlled drug delivery system within the desired region of the gastrointestinal tract (GIT) due to variable gastric emptying and motility. Venlafaxine is an antidepressant and a serotonin and norepinephrine reuptake inhibitor (SNRI). Its active metabolite, desvenlafaxine, works by blocking the reuptake of serotonin and norepinephrine, which are key neurotransmitters in mood regulation. Gastroretentive dosage forms can stay in the gastric region for several hours and significantly prolong the gastric residence time of drugs. Natural materials have been extensively used in drug delivery because they are readily available, cost-effective, eco-friendly, capable of many chemical modifications, potentially degradable, and compatible due to their natural origin. Keywords: Sustained Release Floating Tablets, Venlafaxine,

Formulation and Characterization of Glucosamine Sulphate Potassium Chloride (GSPC) Loaded Emulgel for the Treatment of Osteoarthritis.

Osteoarthritis (OA) is becoming a major medical burden worldwide due to changing lifestyles and aging populations. Osteoarthritis is a disease characterized by a variety of anatomic and physiological changes to joints, including cartilage degradation, bone remodeling, and the formation of osteophytes. These changes cause pain, stiffness, swelling, and limitations in joint function. Glucosamine serves as a fundamental constituent for cartilage, the resilient connective tissue responsible for cushioning joints. Glucosamine Sulphate Potassium Chloride (GSPC) supplementation is widely employed to mitigate symptoms linked to osteoarthritis, a degenerative joint disorder hallmarked by cartilage degradation. Palliative care aims at minimizing pain and disability and improving function, performance, and quality of life. In this study, the emulgel formulation of GSPC was developed and checked for its potential. Currently, OA does not have a definitive treatment. Since conventional dosage forms cannot deliver the active drug content at a predefined target site in a predictable manner throughout the treatment period, a new carrier system is always required. Considering their reduced size, targeting potential, and site specificity, nanocarrier-based approaches could hold an answer to shortcomings associated with conventional routes. Thus, the objective of the current study was to formulate and characterize glucosamine sulphate potassium chloride-loaded emulgel for the treatment of osteoarthritis. Microemulsion of glucosamine sulphate potassium chloride was formulated using a spontaneous emulsification method comprising of oleic acid (oil phase), Tween 80, Tween 20 (surfactant) and PEG 400, Span 80 (co-surfactant), and distilled water (aqueous phase). The microemulsions were evaluated for surface morphology, globule size, poly-dispersibility index (PDI), zeta potential, and viscosity, and the final batch of microemulsions was selected. The optimized microemulsion contained 35% co-surfactant (propylene glycol), 20% surfactant (Tween 20), and 15% oil (oleic acid) and glucosamine sulphate potassium chloride in a dose of 60 mg, which has sufficient drug loading capacity with a droplet size of 182 nm for optimized formulation. The optimized microemulsion formulation was added to gel prepared by Carbopol 934 in a 1:1 (w/w) ratio, leading to the formulation of glucosamine sulphate potassium chloride- containing emulgel. The prepared emulgel was further evaluated for viscosity, drug content, pH, and in-vitro drug release. Emulgel formulation (F6) showed 88% drug release after 6 hours, and it followed the Higuchi model. Glucosamine Sulphate Potassium Chloride (GSPC) is used in the treatment of OA by increasing the production of proteoglycans, which can cause the cartilage to break down. Emulgel formulation (F3) showed 75.41% drug release, and formulation (F6) showed 88% drug release after 6 h. Therefore, it may be concluded that an emulgel of GSPC can be used as a controlled-release dosage form of the drug for local application in OA.

Roles of Fatty Acid Chain Length and Enzyme-Oriented Drug Controlled Release from pH-Triggering Self-Assembled Fatty Acid Conjugated Quetiapine Nanosuspensions.

Quetiapine (QTP) is a first-line antipsychotic drug, but its therapeutic druggability and patient adherence were limited due to high oral dose strength, low bioavailability and physicochemical/biopharmaceutical issues. To investigate the roles of fatty acid chain length and enzyme-oriented QTP controlled release from pH-triggering self-assembled fatty acid conjugated QTP nanosuspensions (NSPs). QTP was conjugated with different chain length fatty acids (C10-decanoic acid, C14-myristic acid, C18-stearic acid) to obtain QTP-fatty acid conjugates (QFCs: QD, QM, QS) by exploiting 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide/4-dimethylaminopyridine (EDC/DMAP) conjugation chemistry. Then, the solubility, partitioning coefficient (log P), cell viability and cleavage kinetics of QFCs were evaluated. The pH-triggering self-assembled behaviors of QFCs to form QTP-fatty acid NSPs (QDN, QMN, QSN) by varying pH, QFC concentration and proton-to-QTP ratios were characterized. The morphological images, critical micelle concentration (CMC), physicochemical properties and enzyme-oriented QTP controlled release of NSPs were examined. Three QFCs were synthesized with different chain length fatty acids from QTP after desalting fumarate from QTP fumarate. The pH, QFC concentration and proton-to-quetiapine molar ratio could influence physicochemical properties and nanonization behaviors of QFCs. All three QFCs showed no effect on the viability of myoblast cells. The pH-triggering self-assembly of amphiphilic QFCs to form nanoparticles (NPs) occurred as the amine moiety of QTP was readily ionized in a strongly acidic environment (pH 1.2). Interestingly, the longer the fatty acid chain length, the lower water solubility, the higher log P (lipophilicity) and the smaller NP particle size were observed. The conversion rate of QFCs to liberate QTP by esterase in human plasma and liver S9 fractions was also inversely proportional to the fatty acid carbon chain length. Interestingly, the freeze-dried QMN showed the esterase-oriented controlled release of QTP over one month, unlike the initial burst release of QDN or the slowly delayed release pattern of QSN. A new pH-triggering self-assembled nanonization platform was developed using different chain length fatty acid conjugated QTP in low pH environment. By varying fatty acid chain length, the enzyme-oriented QTP controlled release dosage form was challenged to enhance the therapeutic effectiveness of QTP.

Fabrication of Novel Floating 3D-Printed Devices with Adjustable Releasing Channels for Controlled Release

Gastro-retentive drug delivery systems (GRDDS) have been used to improve the therapeutic efficacy of drugs with narrow absorption windows, unstable in alkaline pH, soluble in acidic conditions, and active locally in the stomach. This study aimed to produce a novel floating three-dimensional (3D)-printed device (F3D) from polylactic acid filaments using a fused deposition modeling 3D printer. There were two parts of F3D: a cap with an air chamber for floating property and a body with 6 channels for controlled release. The device was designed to have adjustable channels for the releasing control and gastric retention of Bromhexine, carvedilol, and theophylline. The releasing channels could be adjusted by rotating the base to open or close the number of releasing channels as 3 levels (2, 4, and 6 channels). Morphology, weight variation, ex vivo floating time, and drug release characteristics were examined. The F3D had a smooth texture with a narrow SD value of weight variation and actual size, suggesting that the F3D had high accuracy and consistent fabrication using 3D printing technology. All tablets incorporated F3D was able to float for at least 24 h. Decreasing the number of channels on the devices led to the sustained release of drugs following 2> 4> 6 channels. Hence, F3D could be useful in controlling drug release for various commercial tablets. Keywords: 3D-printed device, Floating device, Fused deposition modeling, Gastroretentive drug delivery systems, controlled release dosage form

A Cutting-Edge Method for Regulated Drug Delivery - Microencapsulation

Microencapsulation is the process of encasing, coating, or surrounding a very small droplet of particle, such as a solid, liquid, or even a gas, with a polymeric particle. In comparison to other parenteral controlled release dosage forms, such as macro-sized implants, microparticles offer a number of important benefits as drug delivery systems, including I an efficient protection of the encapsulated active agent against (e.g. enzymatic) degradation, (ii) the ability to precisely control the release rate of the incorporated drug over periods of hours to months, (iii) an easy administration, and (iv) desired, pre-programmed drug release. There are various methods to chemically encapsulate the substance, including the coacervation approach, the polymeric-polymeric incompatibility method, and the physical method, which include the centrifugal extrusion process, pan coating, spray drying, and the air suspension method. Core material, which is the required substance to be coated, and coating material are the most crucial materials utilised in microencapsulation (which is capable of forming film). Because it applies to the pharmaceutical, agricultural, food, and construction industries. Due to its precise action and minimal adverse effects, it is a better drug delivery technique than conventional drug delivery systems.

Evaluating the Release of Different Commercial Orally Modified Niacin Formulations In Vitro.

To evaluate the release profile of different modified-release oral formulations of niacin, such as immediate-release (IR) powder and tablets, timed-release (TR) caplets, extended-release (ER) capsules, and controlled-release (CR) tablets, to assure their defined release pattern and correlate this release with their matrix polymers. Niacin is used to manage hyperlipidemia by reducing cutaneous flushing and hepatotoxicity adverse events. The release profiles of different types of modified-release dosage forms depend on the types of coating materials (polymers) used in the matrix formation. Although different types of niacin formulations exist, none of the niacin dissolution profiles have been evaluated and compared in the literature. Four commercial orally modified-release niacin brands were collected from a local CVS pharmacy retail store, in Miami, FL, USA. The in vitro release study was conducted in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) conditions. The results of the release patterns of four niacin-modified dosage forms (IR, ER, TR, and CR) were aligned with their release definitions. However, the CR dosage form did not follow an ideal release pattern. The release rate of niacin in vitro was pH dependent, which was confirmed by the similarity factor (f2) results. All the f2 comparison values were below 50 in both the SIF and SGF media, while all the comparisons were below the f2 values for all brands in the SIF media.

Bilayer Tablets: A Promising Novel Drug Delivery System

The bilayer tablet heralds a new chapter in the development of controlled-release formulations with a wide range of properties that result in an effective drug delivery technique. Controlled release dosage forms have been commonly used to increase the treatment of a variety of important drugs. Uses of bilayer tablets for anti-inflammatory and analgesic purposes are a unique feature. Bilayer tablets are useful for releasing two medications in sequence, separating two incompatible chemicals, and creating a sustained-release tablet with the first layer of immediate-release as the initial dose and the second layer as the maintenance dose. The bilayer tablet is a more modern technology that corrects the flaws of single-layer tablets. The objective of this paper is to highlight the obstacles that arise during the preparation of bilayer tablets, as well as to suggest solutions to these issues. To better comprehend bilayer tablets, kinds such as single side press, double side press, and bilayer tablet displacement press are discussed, as well as uses, pros, and disadvantages. Its drug companies have become more interested in mixing two or more APIs (active pharmaceutical ingredients) in a single dosage form to improve patient convenience and compliance throughout the last decade. Many pharmaceutical industries are now working on bi-layer tablets for a variety of purposes, including patent extension, therapeutics, and advertising. This article provides an introduction of bilayer tablet technology, highlighting the key benefits of this type of oral dosage form while also describing current issues and developments in production techniques and the quality of products. The current report covers a variety of elements of bilayer tablets.

A STRATEGIC PROCESS DEVELOPMENT AND IN VITRO CYTOTOXICITY ANALYSIS OF PACLITAXEL-LOADED LIPOSOMES

Objective: Liposomes are the controlled-release dosage form that improves the therapeutic efficacy of the drugs, prolongs the duration of action, reduces dosage frequency, and improves patient compliance. Methods: The thin-film hydration method was used to prepare Paclitaxel liposomes. In this process, cholesterol and sodium deoxycholate were used for the formulation, while chloroform and methanol were used as diluents. Percentage (%) drug release study was carried out in phosphate buffer at pH 7.4 in USP apparatus II (Paddle type)Model no VDA-8D, Veego, Mumbai, India. Results: Paclitaxel liposomes of various batches showed a percentage yield ranging from 38 to 84%. It was observed that (Encapsulation efficiency)EE% of Batches B1 to B10 were 0,62.33,59.51,50.21,44.30,82.25,88.95,72.34,77.37 and 70.63 percentage, respectively. Data fitting to the Peppas, Higuchi, 1st-order, and zero-order models was used to examine the optimized liposome (B7) release kinetic mechanism. Data comparison was done using the correlation coefficient (R2). Zero-order had an observed correlation coefficient (R2) of 0.9988, which was greater than that for other models. Therefore, it was clear that the medication was released from the formulation after the zero-order release. Conclusion: The prepared liposomes were subjected to various evaluation parameters like SEM, zeta potential, particle size analysis, drug release study, etc. Data showed that an increased concentration of cholesterol increases the drug release from liposomes. Microscopic images of the B7 batch revealed that liposomes are spherical and have regular surfaces. Formulation B7 shows good results and can be considered an optimized batch that has been selected for further cell line studies. The statistical analysis was used to support the improved formulation.

Development and Characterization of Hydrogel containing Finasteride

The major goal of this study was to create a controlled-release dosage form utilizing a cellulose-based hydrogel that was cross-linked with propylene glycol. Hydrogels were made by crosslinking the polymer Sodium Alginate + Na CMC with propylene glycol, a suitable crosslinking agent. There is no indication of interaction between the medication, polymers, and other excipients, according to an IR and DSC analysis. The hydrogel gave good swelling and controlled release properties due to the cross linking process. The effect of Calcium Chloride concentration on drug content and t75 percent CDR was found to be non-significant based on the findings. However, the influence of Calcium Chloride concentration on swelling index was substantial, indicating that as Calcium Chloride concentration rose, the swelling index of the hydrogel decreased. Again, the effect of response time on drug content and t75 of percent CDR was substantial, implying that as reaction time rose, drug content and t75 of percent CDR of hydrogel increased as well. However, the effect of response time on the swelling index was not statistically significant. Drug content, swelling index, and t75 of percent CDR of run BB1 are the best than compared with based on all responses. This run's drug content, swelling index, and t75 percent CDR are respectively 99.5 percent, 276.64 percent, and 3.5 hrs. So BB1 was used to test the improved formulation, which produced the best in vitro release of 94.24 percent in 6hrs. Different kinetic models were fitted to the in vitro data which showed the best model was higuchi with non-fickian mode of drug release and stability data showed that the formulations were stable during the time span of the study. From the study it was concluded that the prepared hydrogel can provide a sustained release effect with better bioavailability which will surely enhance its absorption throughout the body.

Preparation and in vitro release of mPEG-PLA microspheres of Panax notoginseng saponins

This study was performed to promote the clinical application of Panax notoginseng saponins (PNS), which present anti-inflammatory and antitumor activities, and provided insights for the preparation of controlled-release dosage forms of traditional Chinese medicine. A series of drug-loaded microspheres with degradable amphiphilic polymer material polyethylene glycol monomethyl ether-polylactic acid (mPEG-PLA) as the carrier was synthesized. The degradation, sustained-release behavior, and biocompatibility of the drug-loaded microspheres were studied through in vitro release, degradation, hemolysis, anticoagulation, and cytotoxicity experiments. The pharmacological activities of the microspheres were studied through anti-inflammatory and antitumor experiments. The results showed that the best carrier material was mPEG2k-PLA (1:9), with an average particle size of 3.47 ± 0.35 μm, a drug load of 5.50 ± 0.28 %, and an encapsulation efficiency of 38.52 ± 1.93 %. This material could be released stably for approximately 24 days and degrade in approximately 60 days. Moreover, the microspheres had good biocompatibility and anti-inflammatory and antitumor activities.

Biocompatible Supramolecular Mesoporous Silica Nanoparticles as the Next-Generation Drug Delivery System.

Supramolecular mesoporous silica nanoparticles (MSNs) offer distinct properties as opposed to micron-sized silica particles in terms of their crystal structure, morphology–porosity, toxicity, biological effects, and others. MSN biocompatibility has touched the pharmaceutical realm to exploit its robust synthesis pathway for delivery of various therapeutic molecules including macromolecules and small-molecule drugs. This article provides a brief review of MSN history followed by special emphasis on the influencing factors affecting morphology–porosity characteristics. Its applications as the next-generation drug delivery system (NGDDS) particularly in a controlled release dosage form via an oral drug delivery system are also presented and shall be highlighted as oral delivery is the most convenient route of drug administration with the economical cost of development through to scale-up for clinical trials and market launch.

An Integrative QbD Approach for the Development and Optimization of Controlled Release Compressed Coated Formulation of Water-Soluble Drugs

Controlled release dosage forms maintain regulated pharmacokinetic profile of drug substance within its therapeutic window by ensuring constant plasma concentrations. Controlled release formulations not only increase the therapeutic efficacy of drug substances but also reduce their dose-related side effects. Present investigation was conducted to develop, optimize, and validate compressed coated controlled release tablet formulation for highly water-soluble drug substances which have no rate-controlling factor towards its release from dosage form. Drug dispersed waxy core tablet, press coated within the swellable hydrophilic polymeric barrier layer, was developed and optimized via quality by design approach (QbD) using Box-Behnken design. The optimized formulation was characterized and validated using in vitro quality control parameters. Attributes identified under SUPAC guidelines, such as drug release rates at 30 min, 6 h, and 12 h, were considered as the critical quality attributes (CQAs) that significantly affected efficiency of the compressed coated controlled release tablets. CQAs screened using risk assessment and Pareto chart analyses were used for optimizing controlled release dosage form. Findings revealed that tablets containing drug to wax ratio of 1:1, hydrophilic swellable polymer concentration of 200 mg, and prepared using compression pressure of 6.5 kg/cm2 exhibited the highest desirability indices in terms of controlling the release rate of drug substance. Optimized formulation was also evaluated for swelling rate, erosion rate, and other post-compression parameters, including release kinetics. Fickian diffusion-based zero-order controlled release of BCS class I drug substance was achieved through the developed dosage form.

Controlled metoprolol tartrate release from poly(ε-caprolactone)-poly(ε-caprolactone)/polyethylene oxide/metoprolol tartrate composites with alternating multi-layered structures prepared through layer-multiplying co-extrusion

Multi-layered structure design has provided a promising and powerful strategy for the fabrication of controlled-release dosage forms. However, a convenient and effective preparation technology is still urgently needed. Herein, we applied layer-multiplying co-extrusion (LMCE) technology to construct poly(ε-caprolactone)-poly(ε-caprolactone)/polyethylene oxide/metoprolol tartrate (PCL-PCL/PEO/MPT) composites with alternating multi-layered structures in one step. The layer number could be doubled by an addition of layer-multiplying element. The degradation analysis indicated that fewer PCL layers were beneficial to the dissolution of PEO and increased the pore size in the matrix. The in vitro release results suggested the MPT encapsulated in PEO aggregates was released gradually in a layer-by-layer manner, and the MPT release was flexibly modulated by the number of PCL layer and PEO content. Additionally, methyl thiazolyl tetrazolium assay presented a potential application of PCL-PCL/PEO/MPT composites in tissue engineering. The LMCE technology should have great potential for the preparation of controlled-release dosage forms.

Recent Trends in Assessment of Cellulose Derivatives in Designing Novel and Nanoparticulate-Based Drug Delivery Systems for Improvement of Oral Health.

Natural polymers are revolutionizing current pharmaceutical dosage forms design as excipient and gained huge importance because of significant influence in formulation development and drug delivery. Oral health refers to the health of the teeth, gums, and the entire oral-facial system that allows us to smile, speak, and chew. Since years, biopolymers stand out due to their biocompatibility, biodegradability, low toxicity, and stability. Polysaccharides such as cellulose and their derivatives possess properties like novel mechanical robustness and hydrophilicity that can be easily fabricated into controlled-release dosage forms. Cellulose attracts the dosage design attention because of constant drug release rate from the precursor nanoparticles. This review discusses the origin, extraction, preparation of cellulose derivatives and their use in formulation development of nanoparticles having multidisciplinary applications as pharmaceutical excipient and in drug delivery, as bacterial and plant cellulose have great potential for application in the biomedical area, including dentistry, protein and peptide delivery, colorectal cancer treatment, and in 3D printable dosage forms.

Formulation and Evaluation of Mucoadhesive Floating Microspheres of Repaglinide

The main objective of the present study was to design a controlled release dosage form for an oral anti diabetic drug i.e. repaglinide employing polymers like eudragit s- 100. One of the other objective of this present study was to increase the biological half-life the drug by formulating into microspheres. The microspheres of repaglinide were prepared by solvent evaporation method by using eudragit s-100 and ethyl cellulose as polymers with different concentrations. Formulations (F1-F10) were prepared and evaluated for various micrometric properties and it was observed that though all the formulations were exhibited good flow properties, The F5 formulation exhibits higher in- vitro buoyancy time and entrapment efficiency which is considered for in- vitro and mucoadhesive studies. The FTIR results reveal that there was no interaction between the drug and the excipients. The in- vitro release profiles of F1-F5 indicated that all formulations showed controlled release over an extended period, with acceptable release kinetics. Among the all formulations F5 were considered as a promising candidate for sustain release of repaglinide.