Applications of polysaccharides in topical and transdermal drug delivery: A recent update of literature

Abstract The main aim of transdermal drug delivery (TDD) is to deliver a specific dose of drug across the skin and to reach systemic circulation at a controlled rate. On the other hand skin is the target for topical drug delivery. Mentioned drug delivery systems (DDS) have numerous advantages compared to oral and parenteral routes. Avoidance of first-pass metabolism, prevent drug degradation due to harsh environment of the stomach, allow controlled drug delivery, provide patient compliance, and pain-free administration are a few of them. To achieve all of them, a DDS with suitable polymer is the primary requisite. Based on the recent trends, natural polymers have been more popular in comparison to synthetic polymers because the former possesses favourable properties including nontoxic, biodegradable, biocompatible, low cost, sustainable and renewable resources. In this context polysaccharides, composed of chains of monosaccharides bound together by glycosidic bonds, have been successfully employed to augment drug delivery into and across the skin with various formulations such as gel, membrane, patches, nanoparticles, nanofibres, nanocomposite, and microneedles. In this chapter, various polysaccharides such as cellulose, chitosan, and their semisynthetic derivatives, alginate, pectin, carrageenan etc, were discussed with their diverse topical and TDD applications. In addition, various formulations based on polysaccharides and limitations of polysaccharides were also briefly discussed.

Advances in the research of protein nanocarrier materials / 中国药科大学学报

@#Nanotechnology has brought new strategies in the area of pharmaceutical sciences, especially in the drug delivery system. Among them, the application of protein as drug carriers has drawn extensive attention. A wide variety of proteins that have been used fordrug delivery system including the common animal- and plant-basedproteins, as well as the recombinant protein nanoparticles, which possess many advantages such as biocompatibility, biodegradability, low antigenicity, higher stability and drug loading property. This system is of great significance in the fields of clinical treatment, especially targeted therapy of tumors. In this paper, the fabrication of nanoparticles from animal, botanical, and recombinant proteins are described. And then, trend of development in protein-based nanocarriers is also prospected.

Desenvolvimento e caracterização de filme biodegradável inteligente à base de amido de banana verde e extrato de brassica oleraceae (repolho roxo) / Development and characterization of green biodegradable film based on green banana starch and brassica oleraceae extract (purple cabbage)

O objetivo deste estudo foi desenvolver e caracterizar filme indicador de qualidade de alimentos utilizando amido de banana verde incorporado com extrato de repolho roxo. Os filmes foram desenvolvidos a partir de duas formulações: i) amido de banana sem extrato; ii) amido de banana com extrato. Os filmes foram caracterizados através de análise térmica (TG/DT), ensaio mecânico, espectroscopia por infravermelho (FT-IR), índice de intumescimento e ativação em diferentes pH. Os filmes apresentaram um perfil similar de perda de massa, indicando pouco efeito da incorporação do extrato à sua estabilidade térmica. A incorporação do extrato vegetal promoveu maior resistência mecânica e menor taxa de intumescimento. FT-IR mostrou que não houve interação do extrato com o biopolímero. O filme de amido apresentou sensibilidade à variação do pH. O uso do amido de banana verde combinado com gelatina e extrato de repolho roxo apresenta potencial aplicação como indicador visual de qualidade de alimentos duranteo armazenamento.

The aim of the study was to develop and characterize food quality indicator film using green banana starch incorporated with purple cabbage extract. The films were developed from two formulations: i) banana starch without extract; ii) banana starch with extract. The films were characterized by thermal analysis (TG/DTA), mechanical assay, infrared spectroscopy (FT-IR), swelling index and activation at different pH. The films presented a similar profile of mass loss, indicating that extract did not affect thermal stability. The incorporation of the vegetal extract promoted greater mechanical resistance and a lower rate of swelling. FT-IR showed that there was no interaction of the extract with the biopolymer. The starch film showed sensitivity to pH variation. The use of green banana starch combined with gelatin and purple cabbage extract has potential application as a visual indicator of food quality during storage.

Yield and rheological properties of exopolysaccharide from a local isolate: Xanthomonas axonopodis pv. vesicatoria

Background: The aim of the present study was to evaluate gum productivity of a local strain, Xanthomonas axonopodis pv. vesicatoria, isolated from pepper plant, and its rheological behavior for the first time compared to the standard strain, Xanthomonas campestris DSM 19000 (NRRL B-1459). The influence of operational conditions (agitation rate and inoculum volume) on gum production and rheological properties of gums from the Xanthomonas strains were investigated. Results: The isolated strain of Xanthomonas showed similar xanthan yield compared to the standard strain. Furthermore, this study clearly confirmed that gum yield depended on bacterial strain, agitation rate, and inoculum size. The most suitable conditions for the gum production in an orbital shaker in terms of agitation rate and inoculum size were 180 rpm and 5%, respectively, resulting in an average production of 10.96 and 11.19 g/L for X. axonopodis pv.vesicatoria and X. campestris DSM 19000, respectively. Regarding the rheological properties, Ostwald-de-Waele and power law models were used to describe flow and oscillatory behavior of the gum solutions, respectively. Consistency of the novel gum solution remarkably was much higher than the commercial xanthan gum solution. Flow and oscillatory behavior and their temperature ramps showed that weak gel-like structure could be obtained with less gum concentrations when the novel gum was used. Conclusion: Therefore, yield and technological properties of the aqueous solutions of the exopolysaccharide synthesized by X. axonopodis pv. vesicatoria were observed to be more suitable for industrial production.

In vivo mucoadhesive strength appraisal of gum Manilkara zapota

The mucilage (MMZ) extracted from the seeds of Manilkara zapota(Linn.) P. Royen syn. using maceration techniques was evaluated for mucoadhesive strength by various in vitro and in vivo methods. The result showed that mucoadhesive strength of seeds mucilage have comparable property toward natural and synthetic polymers such as Guar Gum and hydroxyl propyl methyl cellulose (HPMC E5LV) under the experimental conditions used in this study. Briefly, it could be concluded that the seed mucilage of Manilkara zapota can be used as a pharmaceutical excipient in oral mucoadhesive drug delivery systems. Further, it may be appropriate to study the changes in these properties after chemical modifications.

Mucilagem (MMZ) extraída das sementes de Manilkara zapota(Linn.) P. Royen syn utilizando técnicas de maceração foi avaliada por sua força mucoadesiva por vários métodos in vitro e in vivo. O resultado mostrou que a força mucoadesiva das sementes mucilaginosas tem propriedade comparável aos polímeros naturais e sintéticos, tais como goma Guar e hidroxipropilmetil celulose (HPMC E5LV) nas condições experimentais utilizadas neste estudo. Brevemente, se pode concluir que a mucilagem de semente de Manilkara zapota pode ser usada como um excipiente farmacêutico em sistemas de liberação de fármacos mucoadesivos por via oral. Pode ser apropriado o estudo posterior de mudanças nessas propriedades após modificações químicas.

Formulation and in-vitro bioequivalence evaluation of verapamil hydrochloride matrix tablets with Calan SR.

The purpose of the current work was to formulate Verapamil Hydrochloride (VH) sustained release matrix tablets by using natural polymers and comparison with leading national brand Calan SR of Searle Pharmaceuticals. Tragacanth and pectin were used in various concentrations. Pre compression studies i.e. angle of repose, bulk density, tapped density, Carr’s compressibility index and Hausner’s ratio were also performed and found within the Pharmacopoeial limits. Eight formulations (F1-F8) of (VH) were prepared by direct compression method. Post compression studies i.e. Thickness, Hardness, Diameter, Friability and Dissolution studies were conducted. Different kinetic models i.e. zero order, first order, Highuchi model and Korsmeyer Peppas were applied to study release patterns and similarity index was calculated. Dissolution studies were carried out in phosphate buffer of pH 6.8 showed that formulations (F4 and F8) formulated with higher polymers concentration showed comparatively better drug retardation. F5 was the most comparable with the reference product. Verapamil hydrochloride released was observed non-fickian as diffusion following Higuchi model.

Design and Evaluation of Imatinib Mesylate Loaded Microspheres for Stomach Specific Drug Delivery.

Aims: The aim of the present work was to design and evaluate the Imatinib mesylate microspheres using natural and semi synthetic polymers for stomach specific drug delivery. Study Design: Design and Evaluation of Imatinib Mesylate loaded microspheres Place and Duration of the Study: The study was carried out in Department of Pharmaceutics, JKKMMRF’s Annai JKK Sampoorani Ammal College of Pharmacy, between November 2012 and July 2013. Methodology: The microspheres were prepared using Sodium alginate as a polymer by Emulsification Ionic Gelation Technique. Copolymers of natural origin namely Guar gum, Karaya gum, Chitosan and semi synthetic origin namely Hydroxy propoylmethyl cellulose K4M, K15M, K100M are used as mucoadhesive polymers. The prepared microspheres were evaluated for their percentage yield, entrapment efficiency, degree of swelling, particle size, surface morphology and in-vitro mucoadhesion, drug release studies. Drug release kinetics was determined from drug release data. Selected formulations are subjected to stability studies under varying conditions of temperature and humidity. Results: The production yields of microspheres were found to be between 76.74 to 88.18%. Percentage drug entrapment efficiency of Imatinib mesylate microspheres was ranged from 65.51 to 88.78%. Particle size of the prepared microspheres was in the size range of 440-810μm. SEM analysis revealed that all the prepared microspheres were discrete, spherical in shape. The in-vitro mucoadhesive study demonstrated that Hydroxy propoylmethyl cellulose adhered to the mucus to a greater extent than other polymers. The in-vitro release study shows that, retarded release with increase in percentage of polymers. The release of drug from the microspheres followed Krosmeyer Peppas kinetics. After the stability studies, the formulations remained stable at the end of storage period. Conclusion: Based on the results, it was concluded that, the formulations with natural polymers were found to be best than semi synthetic polymers for the oral delivery of Imatinib mesylate.

Preparation and characterization of microcapsules of Pterodon pubescens Benth. by using natural polymers

An oleaginous fraction obtained from an alcohol extract of the fruit of Pterodon pubescens Benth. (FHPp) was microencapsulated in polymeric systems. These systems were developed using a complex coacervation method and consisted of alginate/medium-molecular-weight chitosan (F1-MC), alginate/chitosan with greater than 75% deacetylation (F2-MC), and alginate/low-molecular-weight chitosan (F3-MC). These developed systems have the potential to both mask the taste of the extract, and to protect its constituents against possible chemical degradation. The influence of the formulation parameters and process were determined by chemical profiling and measurement of the microencapsulation efficiency of the oleaginous fraction, and by assessment of microcapsule morphology. The obtained formulations were slightly yellow, odorless, and had a pleasant taste. The average diameters of the microcapsules were 0.4679 µm (F2-MC), 0.5885 µm (F3-MC), and 0.9033 µm (F1-MC). The best formulation was F3-MC, with FHPp microencapsulation efficiency of 61.01 ± 2.00% and an in vitro release profile of 75.88 ± 0.45%; the content of vouacapans 3-4 was 99.49 ± 2.80%. The best model to describe the release kinetics for F1-MC and F3-MC was that proposed by Higuchi; however, F2-MC release displayed first-order kinetics; the release mechanism was of the supercase II type for all formulations.

Uma fração oleaginosa obtida do extrato etanólico de frutos de Pterodon pubescens Benth (FHPp) foi microencapsulada em um sistema polimérico. Estes sistemas foram desenvolvidos utilizando o método de coacervação complexa, constituído de alginato/quitosana massa molecular média (F1-MC), alginato/quitosana com desacetilação superior a 75% (F2-MC) e alginato/quitosana de massa molecular baixa (F3-MC). Estes sistemas desenvolvidos têm o potencial tanto de mascarar o sabor do extrato, quanto de protegê-lo de possível degradação química. A influência dos parâmetros de formulação e processo foram determinadas por caracterização química, determinação da eficiência de microencapsulação da fração oleaginosa e por avaliação morfológica da microcápsula. As formulações mostraram-se ligeiramente amareladas, inodoras e com sabor agradável. Os diâmetros médios das microcápsulas foram de 0,4679 µm (F2-MC), 0,5885 µm (F3-MC) e 0,9033 µm (F1-MC). A melhor formulação foi F3-MC, considerando-se que apresentou eficiência de encapsulação de 61,01 ± 2,00%, e perfil de liberação in vitro de 75,88 ± 0,45%; o conteúdo dos vouacapanos 3-4 foi 99,49 ± 2,80%. O melhor modelo para descrever a cinética de liberação foi o modelo proposto por Higuchi para F1-MC e F3-MC, entretanto, para F2-MC foi o modelo de primeira ordem, e o mecanismo de liberação foi do tipo super caso II para todas as formulações.

Formulation and in-vitro bioequivalence evaluation of verapamil hydrochloride matrix tablets with Calan R.

The purpose of the current work was to formulate Verapamil Hydrochloride (VH) sustained release matrix tablets by using natural polymers and comparison with leading national brand Calan SR of Searle Pharmaceuticals. Tragacanth and pectin were used in various concentrations. Pre compression studies i.e. angle of repose, bulk density, tapped density, Carr’s compressibility index and Hausner’s ratio were also performed and found within the Pharmacopoeial limits. Eight formulations (F1-F8) of (VH) were prepared by direct compression method. Post compression studies i.e. Thickness, Hardness, Diameter, Friability and Dissolution studies were conducted. Different kinetic models i.e. zero order, first order, Highuchi model and Korsmeyer Peppas were applied to study release patterns and similarity index was calculated. Dissolution studies were carried out in phosphate buffer of pH 6.8 showed that formulations (F4 and F8) formulated with higher polymers concentration showed comparatively better drug retardation. F5 was the most comparable with the reference product. Verapamil hydrochloride released was observed non-fickian as diffusion following Higuchi model.

Production and characterization of alginate-starch-chitosan microparticles containing stigmasterol through the external ionic gelation technique

Stigmasterol - a plant sterol with several pharmacological activities - is susceptible to oxidation when exposed to air, a process enhanced by heat and humidity. In this context, microencapsulation is a way of preventing oxidation, allowing stigmasterol to be incorporated into various pharmaceutical forms while increasing its absorption. Microparticles were obtained using a blend of polymers of sodium alginate, starch and chitosan as the coating material through a one-stage process using the external gelation technique. Resultant microparticles were spherical, averaging 1.4 mm in size. Encapsulation efficiency was 90.42% and method yield 94.87%. The amount of stigmasterol in the oil recovered from microparticles was 9.97 mg/g. This technique proved feasible for the microencapsulation of stigmasterol.

O estigmasterol, um fitoesterol com diversas atividades farmacológicas, é suscetível à oxidação quando exposto ao ar, calor e umidade. Neste contexto, a microencapsulação é uma forma de proteção contra oxidação, permitindo a incorporação do estigmasterol em diversas formas farmacêuticas e aumentar sua absorção. As micropartículas foram obtidas por gelificação iônica externa, em uma etapa, utilizando como revestimento polímeros naturais de alginato de sódio, amido de milho e quitosana. As micropartículas apresentaram formato esférico com tamanho aproximado de 1,4 mm. O rendimento foi de 94,87% e a eficiência média de encapsulação de 90,42%. A quantidade de estigmasterol no óleo recuperado das micropartículas foi de 9,97 mg/g. O método mostrou-se viável para a microencapsulação do estigmasterol.