Traditional Dosage Research Articles

Mucoadhesive Drug Delivery Systems: A Review of Recent Developments

Purpose: The aim of this article is to present a review of mucoadhesion drug delivery systems. The review covers the mucoadhesive concepts, polymers used, theories and mechanisms of mucoadhesion, and factors affecting the mucoadhesive dosage forms. Study Design: An extensive review was carried out on mucoadhesion formulations, applications, mechanisms, theories, and polymers used in these dosage forms. Results: Mucoadhesive drug delivery system can interact with the mucus membrane, which covers the mucin molecules and mucosal epithelial surface. This interaction leads to an increment of the dosage form residence time at the site of absorption and hence increasing the bioavailability, efficacy of drugs, and improving therapeutic outcomes. Polymers are used to provide muco-adhesion of the dosage form, enhancing drug release pattern, solubility and dissolution of inadequately soluble drugs. Conclusion: Mucoadhesive drug delivery systems were found to be the best alternative approaches for the traditional dosage forms to enhance bioavailability of poorly soluble drugs and to avoid GIT degradation and first pass metabolism of some drugs.

Transdermal Delivery of Salmon Calcitonin Using a Dissolving Microneedle Array: Characterization, Stability, and In vivo Pharmacodynamics.

Salmon calcitonin (sCT) is a polypeptide drug, possessing the ability to inhibit osteoclast-mediated bone resorption. Just like other bioactive macromolecules, sCT is generally administered to the patients by either injection for poor compliance or through nasal spray for low bioavailability, which limits its use as therapeutic drugs. In the present study, to overcome the limitations of the conventional routes, two new dissolving microneedle arrays (DMNAs) based on transdermal sCT delivery systems were developed, namely sCT-DMNA-1 (sCT/Dex/K90E) and sCT-DMNA-2 (sCT/Dex-Tre/K90E) with the same dimension, meeting the requirements of suitable mechanical properties. An accurate and reliable method was established to determine the needle drug loading proportion in sCT-DMNAs. The stability study exhibited that the addition of trehalose could improve the stability of sCT in DMNA under high temperature and humidity. Further, in vivo pharmacodynamic study revealed that DMNA patch could significantly enhanced relative bioavailability to approximately 70%, and the addition of trehalose was found to be beneficial for sCT transdermal delivery. Therefore, sCT-DMNA is expected to replace traditional dosage form, providing a secure, efficient, and low-pain therapeutic strategy for bone disorders.

Film forming transemulgel- A novel drug delivery system

Film forming transemulgel- A novel drug delivery system - IJCAAP- Print ISSN No: - 2581-5555 Online ISSN No:- 2456-9542 Article DOI No:- 10.18231/j.ijcaap.2020.022, IP International Journal of Comprehensive and Advanced Pharmacology-IP Int J Compr Adv Pharmacol

Development of harmonized HPTLC methods for determination of polyphenolic compounds of tinctures

The tincture is a traditional liquid dosage form for the pharmaceutical market of Ukraine. Today, the range of the tinctures of Ukrainian manufacturers has 21 different items, while only six monographs on different tinctures are included in the State Pharmacopoeia of Ukraine. For standardization of tinctures, different combinations of specific and non-specific physical and chemical methods are used. The high-performance thin-layer chromatography (HPTLC) is a modern and specific chromatographic method, that can be used for the identification of polyphenolic substances responsible for a wide range of pharmacological activities of the tinctures.
 The purpose of the study was to identify and compare chromatographic fingerprints (images of chromatograms and peak profiles from images) of flavonoids and phenylpropanoids of 10 tinctures of Ukrainian production in the harmonized mobile phases, to select for each tincture the specific marker zones, to determine the suitability of the specified chromatographic conditions for standardization of the tincture and the possibility to perform in these conditions the quality control for several different tinctures in-parallel.
 The objects of the investigation were Hawthorn tincture, Peppermint tincture, Sage tincture, Motherwort tincture, Calendula tincture, Sophora tincture, Echinacea purpurea tincture, Valerian tincture, Peony tincture, Eucalyptus tincture. The research was carried out using the HPTLC method in the HPTLC automatic herbal system (CAMAG, Switzerland) on the base of two laboratories.
 For each investigated tincture, the determination and comparison of HPTLC chromatographic fingerprints (images and peak profiles of images) of flavonoids and phenylpropanoids obtained in different harmonized mobile phases were performed.
 In the harmonized chromatographic conditions the difference in separation of the bioactive substances was determined; the characteristic marker substances of the tinctures were identified; the suitability of the mobile phase for individual analysis of the tincture or in-parallel analysis of different tinctures on the same plate were determined; the possibility to replace one mobile phase by another, if needed, was determined.
 Proposed HPTLC methods were developed using modern procedure and approach. These allow to reduce of the scope and time of analysis, optimize the economical and labor costs. The findings are of special importance for the pharmaceutical manufacturers and quality control laboratories that perform analysis on a large scale.

Rospective designing and types of buccal drug delivery system: The Review

Buccal bioadhesive films, releasing topical drugs in the oral cavity at a slow and predetermined rate, provide distinct advantages over traditional dosage forms for treatment of many diseases. The mucosa of the buccal cavity is the most easily accessible transmucosal site. This fast dissolving drug delivery system (FDDS) is suited for the drugs which undergo high first pass metabolism and is used for improving bioavailability with reducing dosing frequency to mouth plasma peak levels, which in turn minimize adverse/side effects and also make it cost effective This article aims to review the recent Designs of buccal patches and their developments in the buccal adhesive drug delivery systems, & Buccal drug delivery is a promising area for continued research with the aim of systemic delivery of orally inefficient drugs as well as a feasible and attractive alternative for non-invasive delivery of potent peptide and protein drug molecules.

An Overview of the Recent Developments and Patents in the Field of Pharmaceutical Nanotechnology.

Compared to traditional dosage methods, the Novel Drug Delivery Systems (NDDS) provide various advantages. In the last few years, the interest shifted to works focused on the novel drug delivery methods for small and large molecular drug carriers utilizing particulate drug delivery systems as well. It is evident from the last decade as observed in increased number of patents in this field that the technology has evolved tremendously. Drug carriers utilized by this novel technology include liposomes, dendrimers, polymeric nanoparticles, magnetic nanoparticles, solid lipid nanoparticles, and carbon nanomaterials. Various forms of polymers have been used in the production of nanocarriers. Nanocarriers are colloidal systems varying in size from 10 to 1000 nm. This technology is now used to identify, manage and monitor numerous diseases and physical methods to alter and enhance the pharmacokinetic and pharmacodynamic properties of specific types of drug molecules. Nanoparticles can be formulated by a number of techniques including ionic gelation, crosslinking, coacervation/precipitation, nanoprecipitation, spray drying, emulsion- droplet coalescence, nano sonication techniques, etc. Several methods are used with which these nanoparticles can be characterized. These methods include nuclear magnetic resonance, optical microscopy, atomic force microscopy, photon correlation spectroscopy and electron microscopy, surface charge, in-vitro drug release, etc. Conclusion: In the present review, the authors have tried to summarize recent advances in the field of pharmaceutical nanotechnology and also focused on the application and new patents in the area related to NDDS.

Nanoparticulate targeted drug delivery systems - A Review

Nanoparticulate drug delivery system are the rapidly developing system, and nanoparticles are present in the size range of 1-100nm. Nanoparticles composed of various thermal, electrical, and optical property. Nanoparticles offers the potential advantages over the traditional dosage forms it is ascribable to the properties of nanoparticles. Nanoparticulate drug delivery system ensures the site-specific delivery of a drug(Targeting drug delivery) and aids in improving the efficacy of the new as well as old drugs and has the potential in crossing the various physiological barriers and also improves the therapeutic index of the drugs and increases the patient compliance. The objectives of this review is to classify the nanoparticles based on the different groups, surface properties of nanoparticles, describe the strategies of drug targeting, the necessity of nanoparticles their general method of preparation, different methods used in characterization, self- assembly and mechanism of drug release in a systemic manner. The potential advantages and limitations of various nanoparticulate drug delivery systems are also discussed elaborately.

ACYCLOVIR-SILICA COMPOSITE AS PLATFORM FOR DEVELOPMENT OF NOVEL ORAL DOSAGE FORM OF DRUG WITH PROLONGED RELEASE

In this work the possibility of creation of novel dosage form of acyclovir based on colloid silica for oral administration, which is capable of long sustained release of the drug is estimated. Clinical practice has shown that the traditional oral dosage form of acyclovir has serious drawbacks, one of which is the rapid elimination of the drug from the body. Colloid silica is recognized as a safe food additive in Russia and around the world. This is of particular importance for the development of drug oral dosage forms. The composite was synthesized by acid-catalyzed sol-gel reactions (hydrolysis and polycondensation) of tetraethoxysilane. The acyclovir solution was introduced into the prehydrolyzed silica sol. In experiments in vitro, a kinetic release profile of acyclovir encapsulated in the silica matrix was obtained. The amount of the released drug was determined spectrophotometrically using a spectrometer Carry 100, Varian, Australia. An experimental simulation of kinetics of the release of acyclovir from the synthesized composite in various sections of the gastrointestinal tract was carried out taking into account the literature data on drug transit time through the sections and medium pH in them. The results obtained in this work showed that the sol-gel encapsulation of acyclovir in silica matrix led to the formation of the acyclovir-silica composite, which is able to maintain the concentration of the drug in various sections of the gastrointestinal tract for 26 h regardless of the medium acidity and transit time of the drug through the sections. Thus, the synthesized composite of acyclovir with silica can serve as a platform for further development of a new oral dosage form of prolonged action.

Gas and high performance thin layer chromatographic based-determination method for quantification of thymol in semisolid traditional dosage forms

The control and standardization process of herbal products is a critical point in preparation of those medicaments. In Traditional Persian Medicine (TPM) literature, out of all the different pharmaceutical dosage forms, Jawarish is a semisolid gastrointestinal dosage form with positive related effects. Jawarish-e-Khuzi, including Zataria multiflora, Lepidium sativum, Trachyspermum ammi, Terminalia chebula, ferrous sulfate, and also honey is one of the popular mentioned traditional oral formulations. However, there have been no noticeable and proven control and standardization for this formulation. In this study, Jawarish-e-Khuzi was prepared based on one of the pharmaceutical textbooks of Traditional Persian Medicine (TPM). Using gas chromatography/mass spectroscopy (GC/MS), the volatile composition of this formulation was analyzed. Subsequently, Gas chromatography/flame ionization detector (GC/FID) and High-Performance Thin-Layer Chromatography (HPTLC) techniques were employed to determine the main component. The GC/MS results showed thymol as the main constituent. In the content determination process via GC/FID, thymol was proved to be 0.02% of the whole preparation. The outcome of HPTLC method also corresponded with that of GC/FID. Based on the method validation parameters, both GC/FID and HPTLC methods are useful for the volatile content determination of semisolid dosage forms.

The vaginal sheet: an innovative form of vaginal film for the treatment of vaginal infections

Objective: To develop and characterize a new form of vaginal film.Significance: This formulation is intended to overcome some known limitations of traditional dosage forms. It has an absorptive intention to control symptoms and to improve the treatment of vaginal infections characterized by excessive fluid. The vaginal sheet is a thick drug delivery system easy to manipulate, nontoxic and composed by biocompatible macromolecules and polymers, such as gelatin and chitosan.Methods: The sheets were prepared by formulating gelatin or chitosan based gels isolated or in combination, in association with a plasticizer. Gels were subsequently lyophilized. Different proportions of polymer:plasticizer were tested. Lactose was used as a surrogate to study powder incorporation in the formulation. All formulations were analyzed regarding their organoleptic characteristics, texture (hardness and resilience), in vitro absorption efficiency of vaginal fluid simulant – VFS (pH 4 and 5), pH and acid-buffering capacity.Results: Different properties were obtained by varying polymer and plasticizer proportions. Combinations including gelatin with propylene glycol showed the best organoleptic characteristics. The best proportions were 4:3 and 4:5. Up to 10% of powder was successfully incorporated in the formulation. Hardness and resilience of formulations were largely dependent on the concentration of plasticizer. Absorption of vaginal fluid was found to be highly efficient, especially at pH 5. Buffering capacity, upon dilution in normal saline and VFS, was generally higher for VFS pH 4.Conclusions: The vaginal sheet is a promising solid drug delivery system able to further incorporate drugs to treat vaginal clinical conditions characterized by excessive fluid.

Formulation and Evaluation of Erythromycin Estolate Loaded Drug Balls

The purpose of research work was to develop and optimize drug balls of erythromycin estolate for oral mucosal delivery of drug for fast delivery of drug and better bio-availability with the aim to treatment of whooping cough with also additional advantages over the traditional dosage forms such as suspension and tablets which takes too much time for release of drug but drug balls release mucoadhesive liquid which shows fast drug release, better bioavailability, avoid hepatic first pass effect and fast action. Sodium alginate based drug balls containing erythromycin estolate were prepared by specific method. Sodium alginate, ethyl cellulose were selected on the basis of formulation of drug balls, mucoadhesive force, In-vitro drug release. A 32 factorial design was employed for preparation of drug balls wherein the concentration of sodium alginate, concentration of ethyl cellulose were selected as independent variables while in vitro drug release and percentage permeation were the dependent variables. Drug balls were evaluated with respect to the percentage mucoadhesion, drug content, invitro drug release and permeation studies. F4 formulation was optimized with mucoadhesive force, %permeation efficiency and In-vitro drug release. Drug balls were characterized by FTIR and DSC study. Stability study revealed that the formulation was found to be stable.

Pharmaceutico analytical profile of Kushmanda Avaleha and its modified dosage form as Kushmanda granules

Background: Kushmanda Avaleha (KA, confection) has been described in Sharangdhar Samhita as a drug of choice in Raktapitta Chikitsa (hemorrhage). Ayurveda mentioned Five Basic Kalpanas, which are called Panchvidha Kashya Kalpana. Panchvidha Kashya Kalpana has several drawbacks, such as less palatability, shorter shelf life, etc. Hence, to overcome these drawbacks, secondary formulations were developed. Avaleha Kalpana was a secondary formulation developed by using primary formulations, such as Swaras (juice), Kwatha (decoctions), etc. Avaleha formulation was prepared by using herbal medicinal drugs and food articles such as sugar, ghee (clarified butter), honey etc. Administering proper dose of Avaleha is difficult in new era than Avaleha convert into granules form because, considering the changing scenario of the society, converting traditional dosage forms into more palatable, easily absorbable forms without changing desired therapeutic effects becomes need of the hour. In the current study, an attempt has been made to convert KA into granules form, which is the first step toward research on the formulation; hence, the current work was planned. Aim: Analytical study of KA and its modified dosage form as Kushmanda granules (KG)Materials and Methods: Three batches of KA were prepared as per the reference of Sharangdhar Samhita (8/22–28), and the same is converted into granules by adopting standard operative procedures. Result and Conclusion: Loss on drying at 105°C, total ash, acid-insoluble ash, alcohol-soluble extractives, water-soluble extractives, pH, total sugar, reducing sugar, nonreducing sugar, and total fat and moisture content in the range of Avaleha is 2.3%, 0.7%, 0.103%, 71.22%, 77.12%, 4.2%, 78.15%, 68.21%, 5.6%, and 2.92%. The range of granules is 3.1%, 1.2%, 0.36%, 38.09%, 41.2%, 3.53, 80.17, 78.12, 4.5, 0.92, and 3.12, respectively.

Optimization and characterization of novel sustained release supermicro-pellet based dry suspensions that load dexibuprofen

Traditional dosage forms of dexibuprofen extremely limit their clinical applications because of the bitter taste and the frequent drug administration caused by the relatively short half-life of the drug. This study aims to design novel sustained release (SR) supermicro-pellet based dry suspensions that load dexibuprofen, and also optimize the formulations in terms of morphology, release rate, flowability, and physicochemical stability of dosage forms. Drug-loaded pellets were prepared by using a bottom spray fluid bed coating technique using microcrystalline cellulose supermicro-pellets as the core and PVP K30 or Poloxamer 188 as the binder. The drug-loaded pellets were further coated with Kollicoat SR 30D to form SR pellets. The optimal SR dry suspensions are composed of SR pellets, diluent granules, and suspending agents. PVP K30- and Poloxamer 188-based SR pellets release the drug molecules in a SR manner over 8 h and show a high release profile for Poloxamer 188-based pellets. The drug release profile is not affected by the rotation speed of the paddle but shows a distinct pH-responsive behavior. The physical property of dexibuprofen has been changed during the preparation process. The SR dry suspensions (F5, with high amount of xanthan gum in suspending agents and low amount of poloxamer 188 in diluent granules) show high physical stability with the sedimentation rate of 0.8 (Hu/H) within 5 min and good flowability with the angle of repose (θ) at 27°. Low content variations were observed with a value of A+1.80SD ≤ 15, and no significant change was found in the drug content under high humidity and strong light. In conclusion, novel SR supermicro-pellet based dry suspensions have been successfully prepared, and the optimal formulation shows excellent SR, good flowability, content uniformity, and physicochemical stability.

Fabrication and release behavior of nitrapyrin Microcapsules: Using modified melamine-formaldehyde resin as shell material

As a commonly used nitrification inhibitor, nitrapyrin can significantly improve the utilization of nitrogen in soils. However, the effectiveness of the traditional dosage form of nitrapyrin is reduced by soil adsorption. In this study, nitrapyrin was encapsulated into a melamine-formaldehyde resin microcapsule with good dispersion and release behavior using an in situ polymerization method. The nitrapyrin microcapsules were characterized using Fourier transform infrared spectroscopy, thermogravimetric analysis, scanning electron microscopy, transmission electron microscopy, and particle-size analysis. The results indicated that the microcapsules had a spherical-shell structure, a uniform morphology with nanoscale micropores on the surface, and a decent nitrapyrin loading content (67.19%). Tests revealed that the release behavior of the nitrapyrin microcapsules was outstanding and conformed to the double-release kinetic model. These results of this study indicate that the nitrapyrin microcapsules can be applied as nitrification inhibitors with beneficial environmental effects and high efficacy.

Orally Dispersible films a new platform for Drug Delivery System

Orodispersible films are thin films, when in contact with saliva gets rapidly disintegrate and dissolve to release the medication for oral mucosal absorption. The film plays a major alternative approach to conventional oral dosage form like tablets, capsule, syrups. The thin films are considered to be convenient to swallow,self-administrable, rapid disintegration, dissolution and quick onset of effect which make it as a versatile platform for effective drug delivery. Oral disintegrating films have superiority over the tablet formulations because there is no risk of chocking and friability. Compared with the traditional dosage forms this dosage forms give greater advantage as it provides a new way for the pediatrics, geriatrics, bedridden patients etc. Several types of approaches are there for preparation of the films. Mostly solvent casting method is used for the development of orodispersible films. For the development of dosage forms polymers and plasticizers along with other excipients are used. Usually hydrophilic polymers are used for the preparation. The design of the film requires comprehensive knowledge of pharmaceutical and pharmacological properties of drug and polymers along with the manufacturing therefore the aim of the review provide an overview of preparation the film The present review focus on benefit, composition, approaches for formulation and evaluation of the Orally dispersible film.

Poly(3-hydroxyalkanoate)-based drug formulations: the micro- and nanostructure

Biodegradable and biocompatible polymers referred to as polyhydroxyalkanoates (PHAs) are extensively used in the production of pharmaceutical drugs to ensure sustained release, targeted delivery, reduced toxicity, and increased stability of the drug substance. Although the pharmaceutical industry ordinarily exploits chemically synthesized PHAs, bioengineered polymers are also starting to enjoy growing interest. This article focuses on the research and development of drug formulations based on natural PHAs that act as auxiliary substances for antibacterial, anti-inflammatory, anticancer, and hormonal medications, as well as pain killers, and discusses the association between their properties and the micro/nano structure of the synthetic drug. The problems associated with the poor performance of active components in traditional dosage forms can be overcome in PHAs-based formulations.

A Comprehensive Map of FDA-Approved Pharmaceutical Products.

With the increasing research and development (R&D) difficulty of new molecular entities (NMEs), novel drug delivery systems (DDSs) are attracting widespread attention. This review investigated the current distribution of Food and Drug Administration (FDA)-approved pharmaceutical products and evaluated the technical barrier for the entry of generic drugs and highlighted the success and failure of advanced drug delivery systems. According to the ratio of generic to new drugs and the four-quadrant classification scheme for evaluating the commercialization potential of DDSs, the results showed that the traditional dosage forms (e.g., conventional tablets, capsules and injections) with a lower technology barrier were easier to reproduce, while advanced drug delivery systems (e.g., inhalations and nanomedicines) with highly technical barriers had less competition and greater market potential. Our study provides a comprehensive insight into FDA-approved products and deep analysis of the technical barriers for advanced drug delivery systems. In the future, the R&D of new molecular entities may combine advanced delivery technologies to make drug candidates into more therapeutically effective formulations.

Chemical and pharmacological comparison of modern and traditional dosage forms of Joshanda

Recently, a traditional remedy (Joshanda) has been replaced largely by modern ready-to-use dosage forms, which have not been compared to the original remedy. Therefore, the present study aimed to compare a number of modern dosage forms with traditional remedy. Seven brands, 3 batches each, were compared with a Lab-made formulation with reference to analytical (proximate analyses, spectroscopic and chromatographic metabolomes) and pharmacological profiles (anti-inflammatory and antibacterial activities). Chemical and pharmacological differences were found between Lab-made Joshanda and modern dosage forms. Such variations were also found within the brands and batches of modern formulations (p < 0.05). The Lab-made Joshanda showed significantly higher pharmacological activities as compared to modern brands (p ). The results of the present study indicate that modern dosage forms are unstandardised and less effective than the traditional remedy. Characteristic profiles obtained from Lab-made Joshanda may be used as reference to produce comparable dosage forms.

Therapeutic potential of drug delivery by means of lipid nanoparticles: reality or illusion?

Solid lipid nanoparticles (SLN) are colloidal drug carrier systems that contribute several properties required from a sophisticated drug delivery system for increasing drug bioavailability and providing effective therapy. Many advantages of SLN have been reported over traditional dosage forms and their colloidal counterparts in the studies since the early 1990s. They were optimized for oral drug delivery for the first time. The first SLN formulations were produced by reducing the particle size of solid lipid microparticles by spray congealing technique in the late 1980s. Then, studies have been continued investigating for their different administration routes else including parenteral, transdermal, ocular, nasal, respiratory etc. Their foremost qualifications such as their biocompatible nature and high drug entrapment efficiency make them promising colloidal drug carrier systems for the effective treatment of serious disasters like genetic disorders and cancer. In this review, therapeutic potential of drug delivery of SLN and nanostructured lipid carriers (NLC, the second generation of SLN) are summarized considering researches and patents on their administration via different routes and their preparations in the pharmaceutical market.

Formulation and Evaluation of an Iranian Traditional Dosage Form Containing Linum and Ficus for Improvement of Functional Constipation

Formulation and Evaluation of an Iranian Traditional Dosage Form Containing Linum and Ficus for Improvement of Functional Constipation