Self-Emulsifying Drug Delivery Systems: Concept to Applications, Regulatory Issues, Recent Patents, Current Challenges and Future Directions.

Self-emulsifying drug delivery systems (SEDDS) can increase the solubility and bioavailability of poorly soluble drugs. The inability of 35% to 40% of new pharmaceuticals to dissolve in water presents a serious challenge for the pharmaceutical industry. As a result, there must be dosage proportionality, considerable intra- and inter-subject variability, poor solubility, and limited lung bioavailability. As a result, it is critical that drugs intended for oral administration be highly soluble. This can be improved through a variety of means, including salt generation and the facilitation of solid and complicated dispersion. Surfactants, lubricants, and cosolvents may occasionally be found in SEDDS or isotropic blends. Lipophilic drugs, whose absorption is limited by their dissolution rate, have been used to demonstrate the effectiveness of various formulations and techniques. These particles can form microemulsions and suitable oil-inwater emulsions with minimal agitation and dilution by the water phase as they pass through the gastrointestinal tract. This study summarises the numerous advances, biopharmaceutical components, variations, production techniques, characterisation approaches, limitations, and opportunities for SEDDS. With this context in mind, this review compiles a current account of biopharmaceutical advancements, such as the application of quality by design (QbD) methodologies to optimise drug formulations in different excipients with controllable ratios, the presence of regulatory roadblocks to progress, and the future consequences of SEDDS, encompassing composition, evaluation, diverse dosage forms, and innovative techniques for in vitro converting liquid SEDDS to solid forms.

Genotoxic Impurities in Critical Analysis of Product Development: Recent Advancements, Patents, and Current Challenges.

The current review intends to regulate and accurately evaluate genotoxic contaminants in drug substance and drug product method and formulation process development, validation, and degradation pathways. The Quality by Design (QbD) principles can be applied to the systematic evaluation and control of impurities enabled by the development of modern analytical techniques, including the performance of risk assessment, the screening of Critical Process Parameters (CPPs), and the identification of the most influential variables in the optimization of the evaluation and control methods. Current difficulties in removing genotoxic contaminants and the procedures for doing so have been outlined in this review, along with the steps necessary to acquire optimum techniques and the most acceptable formulations. In addition to this, division, characterization, assessment, quantification, and formation of genotoxic impurities sources and control strategy for genotoxic impurities, handling of nitrosamine assay content of drug products in different industrial methodologies and their chemometric prospects and associated recent patents are also explored.

Advancement and Applications of Platelet-inspired Nanoparticles: A Paradigm for Cancer Targeting.

Platelet-inspired nanoparticles have ignited the possibility of new opportunities for producing similar biological particulates, such as structural cellular and vesicular components, as well as various viral forms, to improve biocompatible features that could improve the nature of biocompatible elements and enhance therapeutic efficacy. The simplicity and more effortless adaptability of such biomimetic techniques uplift the delivery of the carriers laden with cellular structures, which has created varied opportunities and scope of merits like; prolongation in circulation and alleviating immunogenicity improvement of the site-specific active targeting. Platelet-inspired nanoparticles or medicines are the most recent nanotechnology-based drug targeting systems used mainly to treat blood-related disorders, tumors, and cancer. The present review encompasses the current approach of platelet-inspired nanoparticles or medicines that have boosted the scientific community from versatile fields to advance biomedical sciences. Surprisingly, this knowledge has streamlined to development of newer diagnostic methods, imaging techniques, and novel nanocarriers, which might further help in the treatment protocol of the various diseased conditions. The review primarily focuses on the novel advancements and recent patents in nanoscience and nanomedicine that could be streamlined in the future for the management of progressive cancers and tumor targeting. Rigorous technological advancements like biomimetic stem cells, pH-sensitive drug delivery of nanoparticles, DNA origami devices, virosomes, nano cells like exosomes mimicking nanovesicles, DNA nanorobots, microbots, etc., can be implemented effectively for target-specific drug delivery.

Clinical Profile and Outcomes of Multisystem Inflammatory Syndrome in Children: A Multicentric Observational Study.

Background and objective Multisystem inflammatory syndrome in children (MIS-C) is a postinfectious, generalized, hyperimmune state and is potentially lethal. There is scarce data on the clinical presentation and epidemiology of MIS-C in India. In light of this, we conducted this study to describe clinical presentations and outcomes in children diagnosed with MIS-C. Methodology This was a 15-month hospital-based prospective observational study conducted in the Departments of Pediatrics at Jagannath Hospital and Hitech Medical College, Bhubaneswar. The study included all patients diagnosed with MIS-C and treated at these hospitals between May 1, 2020, and August 31, 2021. The inclusion criteria were as follows: patients who were reverse transcription-polymerase chain reaction (RT-PCR)-positive, antibody-positive, or had known contact with those infected with coronavirus disease 2019 (COVID-19). We reviewed patient medical records to collect demographic data such as age, sex, body mass index (BMI), duration of illness, clinical symptomatology, findings of initial echocardiography, and outcomes. We followed each case for three months. We analyzed descriptive statistics using percentages and means and conducted the statistical analysis using SPSS Statistics for Windows, Version 25.0. (IBM Corp., Armonk, NY). Results A total of 30 cases were included in the study, consisting of 16 boys (53.3%) and 14 girls (46.7%). The mean age of the study population was 6.7 years, and 43% had a BMI in the overweight range. All patients (100%) had a fever, 66.7% had lethargy (n=20), and 64.3% (n=19) had abdominal symptoms in the form of vomiting, diarrhea, and abdominal pain. Respiratory distress at admission was found in 16 cases (53.3%), while hypotension at admission was found in 18 (60%) cases. Our population's average duration of pediatric ICU stay was 3.7 ± 1.2 days, and the average duration of inotropy was 2.2 ± 0.5 days. Fifteen cases (50%) required only oxygen support; 10 (33%) required noninvasive ventilation, and only one patient required invasive ventilation. Twenty-two patients (74%) needed fluid boluses. Outcomes of coronary artery dilatations were favorable, regressing to normal (Z-score <2.5) in affected patients within 90 days of follow-up. Conclusions MIS-C has myriad presenting signs, symptoms, and severity. It is often associated with circulatory failure or shock. However, most patients demonstrated good early outcomes, improved left ventricle (LV) function, normalization of coronary abnormalities, and no mortality. This study provides additional data on the clinical presentation of MIS-C and highlights the importance of close, long-term follow-up monitoring of this patient population.

Design of experiments assisted the development of inclusion complexes of ramipril using hydrophilic carriers for enhancement of solubility and dissolution rate

Abstract The goal of the present study was to develop inclusion complexes and polymers dispersions of ramipril prepared by physical mixing, kneading, co-evaporation, and solvent evaporation methods to enhance drug solubility and dissolution rate, and thereby to reduce drug dose and side effects using selected hydrophilic carriers such as β-CD, PVP-K25, PEG 4000, and HPMC K100M. The prepared formulations were characterized for solubility and in-vitro drug release studies. The systematic optimization of formulations was performed using I-Optimal experimental design by selecting factors such as type of carriers (X1), drug: carrier ratio (X2), and method of preparation (X3), and response variables including percent yield (Y1), solubility (Y2), Carr's index (Y3) and drug release in 30 min (Y4). Mathematical modeling was carried out using a quadratic polynomial model. The inclusion complex formulation (F27) was selected as an optimized batch by numerical desirability function and graphical optimization with the help of design space. The inclusion complex prepared by the co-evaporation method showed maximum drug solubility and released in pH 6.8 phosphate buffer compared to pure and other formulations. The inclusion complex is a feasible approach to improve the solubility, dissolution rate, bioavailability, and minimization of drugs' gastrointestinal toxicity upon oral administration of ramipril.

QbD-based Formulation Optimization and Characterization of Polymeric Nanoparticles of Cinacalcet Hydrochloride with Improved Biopharmaceutical Attributes

Objectives: The aim of the present work was to prepare QbD enabled optimization, and to improve the oral bioavailability of freeze-dried polymeric nanoparticles of cinacalcet hydrochloride manufactured by nanoprecipitation and ultrasonication methods using polymers PLGA, and poloxamer-188. Materials and Methods: The initial screening and optimization were carried out for the formulations by employing Taguchi and Box-Behnken Designs. The FT-IR and DSC revealed no interactions and had no incompatibility among the selected drug and polymers. The nanoparticles were characterized for % drug release, particle size analysis, zeta potential, PDI, SEM, TEM, P-XRD, TGA, DTA, in vitro, and in vivo drug release study. Results: In vitro drug release study showed sustained release of the drug from the optimized batch by diffusion mechanism. The optimized nanoparticle formulation was recognized by numerical and graphical methods using validation of the experimental model. The optimized batch was stable as per the ICH stability guidelines for 6 months with no considerable alternation noticed in particle size, entrapment efficiency, and in vitro drug release. The pharmacokinetic parameters of AUC and Cmax data for the optimized formulation increased 3- and 2.9-folds compared to the pure-drug suspension. Conclusion: The prepared polymeric nanoparticles formulation is an alternative delivery system for enhanced therapeutic efficacy and bioavailability potential of a model drug to manage long-term normocalcemia in patients with preliminary hyperparathyroidism.

AQbD Driven Development of an RP-HPLC Method for the Quantitation of Abiraterone Acetate for its Pharmaceutical Formulations in the Presence of Degradants.

OBJECTIVES: Abiraterone acetate is a well-known anticancer drug and a steroidal derivative of progesterone for treatment of patients with hormone-refractory prostate cancer. Chemometrics-assisted reverse phase high performance liquid chromatography (RP-HPLC) development of the drug abiraterone acetate has been employed in this study using an analytical quality by design (AQbD) approach. MATERIALS AND METHODS: Drug separation was performed using a Princeton Merck-Hibar Purospher STAR (C18, 250 mm × 4.6 mm) i.d., 5 µm particle size) with ultraviolet detection at 235 nm. A Box-Behnken statistical experimental design with response surface methodology was executed for method optimization and desired chromatographic separation from its formulation with a few numbers of experimental trials. The impact of three independent variables, namely, composition of the mobile phase, pH, and flow rate, on response retention time and peak area was studied by constructing an arithmetic model from these variables. RESULTS: Optimized experimental conditions for the proposed work include the mobile phase acetonitrile and phosphate buffer (10 mM KH2PO4) (20:80 %v/v). At the concentration range of 2-100 µg/mL, a linear calibration curve was found. Recovery was performed at three concentrations and was foun to be between 98% and 102%. The 3D response surface curves revealed that mobile phase composition and flow rate were the most substantial critical factors affecting desired responses. CONCLUSION: An attempt has been made to develop and validate an economical, precise, robust, stability-indicating AQbD-based RP-HPLC method that can be employed successfully for the routine analysis of abiraterone acetate in quality control labs.

Analytical Quality by Design Based Systematic Development and Optimization of a Sensitive Bioanalytical Method for Estimation Cinacalcet HCl in Rabbit Serum.

Context: There is no straightforward method for estimating cinacalcet HCl in biological materials such as serum exists. As a result, the goal of this research is to develop a simple quality by design (QbD) enabled reverse phase-Ultra-Fast Liquid Chromatography (RP-UFLC) model for analyzing cinacalcet HCl in serum. Aim: The current study envisages the development and validation of an isocratic simple, precise, and rapid QbD enabled RP-UFLC method for the quantification of cinacalcet HCl in both solution form and blood samples. Subjects and Methods: The optimum conditions were outlined, selecting three influential factors (CMPs) i.e., mobile phase composition, flow rate, and injection volume. Systematic optimization was performed by 32-Box Benkhen experimental design using response surface methodology. The selected variables are further assessed for observed responses Critical Analytical attributes, i.e., peak area, retention time (Rt), USP Plate count. The optimized method used a chromatographic C18 (100 mm × 4.6 mm i.d) column with mobile phase (acetonitrile and Tetrabutyl Ammonium Hydrogen Sulphate [TBSH]) in the ratio of 1:1, with a flow rate of 1 mL/min with UV at λmax 223 nm. The developed method was found to be specific for cinacalcet HCl, enduring no interference of peaks with an overall analytical Rt of 4.3 min. Results: The Accuracy reported as % recovery was found to be 96.83%-101.32% and 95.18%-102.49% respectively. Inter-day precision (reproducibility) and intra-day precision (repeatability) were found to be 0.22-1.19 standard deviation (SD) and 0.14-2.12 SD respectively. The calibration curve was found to be linear with a regression equation Y = 195.8x + 21852, with R 2 0.999 over a concentration range from 100 to 100,000 ng/mL. Conclusion: The required detection and quantitation limits (Limit of Detection and Limit of Quantitation) values were obtained within the acceptance limit based on S/N ratio which indicates the method was sensitive and rapidity of the method. Further, the developed QbD enabled UFLC method was approved and effectively entreated the blood tests to study the pharmacokinetic parameters which indicate a robust, accurate cost-effective method intended for quality control tool for routine systematic analysis in research labs.

Nucleic acid-loaded lipid-polymer nanohybrids as novel nanotherapeutics in anticancer therapy.

INTRODUCTION: Since decades, cancer is a major public health problem worldwide. The increasing knowledge of molecular and tumor biology has significantly changed the cancer treatment paradigms during the past few years. AREA COVERED: Conventionally, the first-line treatment of solid tumors is their surgical removal followed by chemotherapy and/or radiation treatment. Unfortunately, these approaches often fail, and the patient may discontinue the treatment before the complete eradication of tumors due to therapeutic and toxicological limitations. In this regard, the nucleic acid-based treatment therapy has been widely used in the management of cancer. However, nucleic acid delivery to the target sites is highly challenging because of their molecular size, difficulties to pass cellular membranes, and susceptibility toward enzymatic and/or chemical degradation. EXPERT OPINION: Researchers have now overcome many problems associated with delivering nucleic acids to the target tissues by preventing them from off-target side effects and overcoming rapid degradation and clearance in the bloodstream using the lipid-polymer hybrid nanoparticles (LPHNs). The present review, therefore, aims to provide an overview account on LPNHs, their preparation, characterization, application with special emphasis on intracellular delivery/transfection of nucleic acids in the management of cancer, and key aspects of challenges in its delivery and clinical transition.

Mucoadhesive Multiparticulate Drug Delivery Systems: An Extensive Review of Patents.

Innovations in pharmaceutical research are striving for designing newer drug therapies to eradicate deadly diseases. Strategies for such inventions always flourish with keys and objectives of minimal adverse effects and effective treatment. Recent trends in pharmaceutical technology specify that mucoadhesive drug delivery system is particularly appropriate than oral control release, for getting local systematic delivery of drugs in GIT for an extended interval of time at a predetermined rate. However, it is somehow expensive and unpleasant sensation for some patients, but still it is needful for getting short enzymatic activity, simple administration without pain and evasion of fast pass metabolism. Usually the vehicles employed in drug delivery of mucoadhesive system have a significant impact that draws further attention to potential benefits like improved bioavailability of therapeutic agents, extensive drug residence time at the site of administration and a comparatively faster drug uptake into the systemic circulation. The drug release from mucoadhesive multiparticulates is contingent on several types of factors comprising carrier need to produce the multiparticles and quantity of medication drug contained in them. Mucoadhesion is characterized by selected theories and mechanisms. Various strategies emergent in mucoadhesive multiparticulate drug delivery system (MMDDS) by in-vitro as well as ex-vivo description and characterization are also critically discussed. Apart from these, the primary focus during this review is to highlight current patents, clinical status, and regulatory policy for enhancement of mucoadhesive multi-particulate drug delivery system in the present scenario.

Quality by Design: Concept to Applications.

BACKGROUND: Quality by Design (QbD) is associated with a modern, systematic, scientific and novel approach which is concerned with pre-distinct objectives that not only focus on product, process understanding but also lead to process control. It predominantly signifies the design and product improvement and the manufacturing process in order to fulfill the predefined manufactured goods or final products quality characteristics. It is quite essential to identify the desired and required product performance report, such as Target Product Profile, typical Quality Target Product Profile (QTPP) and Critical Quality Attributes (CQA). METHODS: This review highlighted the concepts of QbD design space, for critical material attributes (CMAs) as well as the critical process parameters that can totally affect the CQAs within which the process shall be unaffected thus, consistently manufacturing the required product. Risk assessment tools and design of experiments are its prime components. RESULTS: This paper outlines the basic knowledge of QbD, the key elements; steps as well as various tools for QbD implementation in pharmaceutics field are presented briefly. In addition to this, quite a lot of applications of QbD in numerous pharmaceutical related unit operations are discussed and summarized. CONCLUSION: This article provides a complete data as well as the roadmap for universal implementation and application of QbD for pharmaceutical products.

Transdermal Evaporation Drug Delivery System: Concept to Commercial Products.

Since two decades or so transdermal route established itself as better alternative to traditional oral route. This is possible due to continuous innovations in transdermal drug delivery (TDD), which not only enables researchers from academia and industry to successfully develop and launch many new pharmaceuticals but also allow to include new classes of drugs that can be developed into transdermal formulations. These successes are achieved due to the use of novel techniques based on either physical or chemical approaches. However, both of these techniques suffer due to their own disadvantages. Comparatively, a simple method of supersaturation to enhance drug permeation across skin has created a new wave of interest. Even though the application supersaturated principle in topical and TDD has been used from 1960s, but proper control of drug release and formation of stable supersaturated states has been the core of intense research in the last decade. Out of various methods used to get supersaturated system, evaporation method is considered as most efficient and practically feasible for TDD. Therefore, in this review concept of supersaturation, selection of solvent system and the mechanism of inhibition of crystallization are discussed. Application of evaporation systems in the development of transdermal formulations such as solutions, semisolids and metered dose therapeutic systems (MDTS) and the commercial evaporative systems are also discussed in this review.

An overview of experimental designs in HPLC method development and validation.

Chemometric approaches have been increasingly viewed as precious complements to high performance liquid chromatographic practices, since a large number of variables can be simultaneously controlled to achieve the desired separations. Moreover, their applications may efficiently identify and optimize the significant factors to accomplish competent results through limited experimental trials. The present manuscript discusses usefulness of various chemometric approaches in high and ultra performance liquid chromatography for (i) methods development from dissolution studies and sample preparation to detection, considering the progressive substitution of traditional detectors with tandem mass spectrometry instruments and the importance of stability indicating assays (ii) method validation through screening and optimization designs. Choice of appropriate types of experimental designs so as to either screen the most influential factors or optimize the selected factors' combination and the mathematical models in chemometry have been briefly recalled and the advantages of chemometric approaches have been emphasized. The evolution of the design of experiments to the Quality by Design paradigm for method development has been reviewed and the Six Sigma practice as a quality indicator in chromatography has been explained. Chemometric applications and various strategies in chromatographic separations have been described.

Nanoemulsion for the Effective Treatment and Management of Anti-tubercular Drug Therapy.

BACKGROUND: Tuberculosis is considered as one of the deadliest diseases of human existence. Since ancient age the treatment of tuberculosis has been highly challenging primarily owing to the pathogenic nature of the Mycobacterium and its diverse spots of localization in human body including lungs, liver, spleen, eye, meninges and lymph nodes. METHODS: The conventional drug therapy employed for the treatment of tuberculosis is not highly satisfactorily owing to low oral bioavailability of the drugs. The evolution of nano-technology recently in few decades has completely revolutionized the treatment of diverse diseases and so is the tuberculosis. Nanotechnology not only possesses enormous potential for improving the biopharmaceutical performance, but also allows the delivery of therapeutic molecules to the desired site of action. Diverse types of nanocarriers have been employed for the treatment of tuberculosis infections. In this regard, nanoemulsions are considered as one of the promising alternatives for augmenting the bioavailability of the antitubercular drugs through oral route for improving their therapeutic efficacy. CONCLUSION: The nanoemulsion loaded with antitubercular drugs can easily cross the biological barriers to reach the systemic circulation and consequently in the target for reducing the load of Mycobacterium tuberculosis. Besides, the lipidic nature of such systems facilitates targeting of the drugs to the lymph nodes, thus improves drug bioavailability and reduction of the dosing frequency. In lieu of this, the present article compiles the basics of nanoemulsions in brief along with an updated account on their applications in delivering antitubercular drugs for enhanced immunization. Moreover, overview of patent literature published in this area has also been included in the manuscript.

Nanoparticles for Cancer Targeting: Current and Future Directions.

The targeting of pharmaceuticals is a rapidly evolving strategy to overcome the difficulties in therapeutic delivery, especially to the tumor site. Unlike traditional drug delivery systems, nanoparticles based compounds attain superior accretion in the tumor site by their active or passive mechanisms. Due to their exclusive properties like small size, large surface-to-volume ratio, tunable surface chemistry, and the ability to encapsulate various drugs, the nano-sized carriers provide longer circulation time; easy penetration into cellular membranes; efficient site-specific targeting. Recent advancements in polymeric- nanomedicines involve targeting of polymer-based nanoparticles (NPs), micelles, polyplexes, dendrimers, polymersomes, drug/protein conjugates and lipid hybrid systems to tumor pathological site. With different functional moieties, NPs improve the performance in terms of targetability, circulation longevity, enhanced intracellular penetration, stimuli-sensitivity, and carrier-mediated visualization. This review highlighted different preparative techniques and types of nanoparticles in the most recent developments in cancer treatment including promising opportunities in targeted; combination therapy; and other medical and biomedical applications. Various delivery strategies and future prospects of nanoparticles are also enlisted. Apart from that, the review discusses the potential advances and targeting of polymeric nanocarriers within the scope of cancer therapeutic system to emphasize it as an auxiliary tool to the customary drug delivery systems.

Liposheres as a Novel Carrier for Lipid Based Drug Delivery: Current and Future Directions.

Researchers are facing challenges to develop robust formulation and to enhance the bioavailability of poorly water-soluble drugs towards clinical applications. The development of new drug molecule alone is not adequate to assure ample pharmacotherapy of various diseases. Considerable results obtained from in vitro studies are not supported by in vivo data due to inadequate plasma drug concentrations. This may occur due to limited drug solubility and absorption. To resolve these problems, development of new drug delivery systems will be a promising approach. One of the promising pharmaceutical strategies is the use of lipospheres drug delivery system to deliver the poorly water-soluble drugs. Therefore, the present review described the methodology for manufacturing of lipospheres and factors influencing the formulation to deliver the drugs to the targeted site. Apart from that, this review also enlisted briefly the various applications of liposphers in medical and biomedical fields and critically discussed the recent patent system.

Design and characterization of cefuroxime axetil biphasic floating minitablets.

Biphasic floating minitablets of cefuroxime axetil were prepared by melt granulation technique using two different grades of gelucire namely 50/13 and 43/01 to maintain constant plasma drug concentration. Loading dose of cefuroxime axetil was formulated as immediate release (IR) minitablets by using hydrophilic grade of gelucire 50/13. Maintenance dose was formulated as floating sustained release (SR) minitablets by using hydrophobic grade of gelucire 43/01. The prepared IR and SR granules were subjected to micromeritic studies and scanning electron microscopy. Fourier transform infrared spectroscopy (FT-IR) study revealed that drug and selected carriers were compatible. In vitro dissolution study of optimized IR minitablets showed more than 85% of loading dose dissolved within 30 min. Optimized SR minitablets showed zero lag time with floating duration more than 12 h. The drug release from SR minitablets was linear with square root of time with non-Fickian diffusion-controlled release. The optimized batch of minitablets was filled into 0 size hard gelatin capsule. In vitro dissolution study for capsule showed an immediate burst release followed by SR up to 12 h. There is no significant change in dissolution data after storage at 40 °C and 75% RH for three months. Microbiological assay of dissolution samples of optimized minitablets filled in capsules showed proportionate increase in inhibition of growth against Escherichia coli up to 12 h samples. In vivo bioavailability study in albino rabbits showed three times improvement in oral bioavailability.

Stabilization and delivery approaches for protein and peptide pharmaceuticals: an extensive review of patents.

Proteins and peptides are the building blocks of human body and act as the arsenal to combat against the invading pathogenic organisms for treatment and management of diseases. Majority of such biomacromolecules are synthesized by the human body itself. However, entry of disease causing pathogens causes misleading in the synthesis of desired proteins for antibody formation. In such alarming situations, the delivery of requisite protein and peptide from external source helps in augmenting the body's immunity. The major drawbacks underlying poor biopharmaceutical performance of high molecular weight protein and peptide drugs are due to poor oral absorption, formulation stability, degradation in the gastric milieu, susceptible to presystemic metabolism. Numerous literature recounts the application of myriad drug delivery strategies for the effective delivery of protein and peptides viz. parentral, oral, transdermal, nasal, pulmonary, rectal, buccal and ocular drug delivery systems. There are many reviews on various delivery strategies for protein and peptide pharmaceuticals, but the present review article provides a bird's eye view on various novel drug delivery systems used for enhanced delivery of protein and peptide pharmaceuticals in the light of patent literature. Apart from this, the present manuscript endeavor provides idea on possible causes and major degradation pathways responsible for poor stability of protein and peptide drugs along with recent market instances on them utilizing novel drug delivery systems.

Osmotic drug delivery systems: basics and design approaches.

Osmotic drug delivery system utilizes the principles of osmotic pressure for the controlled delivery of active pharmaceutical ingredient at a predetermined zero order rate. An appropriately designed osmotic drug delivery is not influenced by different physiologic factors but affected by pharmaceutical factors, which play a pivotal role in modulating the release of drug. The present review critically discussed about the factors affecting drug release from the delivery system such as solubility, osmotic pressure, size of delivery orifice and membrane characteristics. The major arena of this review is to highlight about the different types of osmotic drug delivery systems such as implantable, single chamber, multi chamber osmotic pumps and several specialized type of osmotic pumps. Apart from that this system is a versatile technology useful for delivery of drugs with varying solubility. The additional properties of this delivery system can also exhibit pulsatile release, burst release and colon targeting of drug. Because of its versatility, this above system seems to have promising approach which can result in improved safety profile, stable drug concentrations, uniform drug effects and dosing frequency. Current review also briefly discussed about the patents related to delivery of drugs by the principle osmotic pressure.

Design and characterization of enteric-coated controlled release mucoadhesive microcapsules of Rabeprazole sodium.

The objectives of present work was to design and characterize the rabeprazole sodium loaded microcapsules prepared by solvent evaporation technique using ethyl cellulose (EC) based various mucoadhesive polymer, followed by a triple coating with Eudragit L100. The Box-behnken design (BBD) was applied for optimization of formulations containing EC, HPMCK100M and Eudragit L100 as factors for selected responses like entrapment efficiency, mucoadhesive property and drug release in 24 h. The prepared microcapsules were characterized for particle size, drug content, swelling index, mucoadhesive strength, and in vivo antiulcer activity. FT-IR studies revealed that there was no drug-polymer interaction. SEM studies revealed that microcapsules were non-aggregated, spherical shape and smooth appearance. In vitro drug release data from microcapsules was fitted to different kinetic models to explain release profiles. The correlation coefficient value (r(2)) indicated that the drug release followed Higuchi model. Analysis of variance (ANOVA) showed significant difference in the release of drug from all formulations at p < 0.05 level. Accelerated stability study of optimized formulation (F4) upto 6 months showed there was no change in drug content and release characteristics during storage. In vivo antiulcer activity showed that the optimized microcapsules were able to protect rat stomach against ulcer formation vis-à-vis aqueous solution of the drug showed only negligible and minimum effect.