pH Dependent Release Potential of Natural Polymers in Sustained Release of Ornidazole From Colon Targeted Delivery System)

2019 ◽  
Vol 9 (02) ◽  
Author(s):  
Sharma Pankaj ◽  
Tailang Mukul
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Targeted Delivery ◽  
Guar Gum ◽  
Acidic Environment ◽  
Natural Polymers ◽  
Weight Variation ◽  
Curve Determination ◽  
Preformulation Studies

The aim of present work was to prepare colon specific delivery system of Ornidazole using different ratio of shellac, zein and guar gum. From study of various literature it revealed that shellac, zein and guar gum released drug from dosage form at the pH of 6.9, 11.5, 7-9 respectively. The main problem associated with colon targeted drug delivery system is degradation of drug in the acidic environment of stomach to circumvent the present problem different combinations of shellac, zein and guar gum were employed in the formulation of colon targeted tablet. Several preformulation parameters were determined such as melting point, FTIR spectroscopy, preparation of calibration curve, determination of λmax and partition coefficient. After the preformulation studies, next steps were preparation of core tablets, evaluation of core of tablets and coating of tablets. The data obtained from preformulation study seven formulations were developed and evaluated for various parameters. Based on evaluated parameter such as weight variation, friability, dissolution study, invitro drug release etc. the F7 formulation show better results colon targeted tablets. Drug content in F7 formulation was 95% and drug release after 6 hrs was 96%. Formulation containing combination of shellac, zein and guar gum released least amount of drug in the acidic environment of stomach and released most of the drug in colon. It is evide

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEM FOR RITONAVIR TABLETS USING NATURAL POLYMERS

2017 ◽  
Vol 10 (5) ◽  
pp. 318
Author(s):  
Saritha Chukka
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Guar Gum ◽  
Prolonged Release ◽  
Natural Polymers ◽  
Drug Bioavailability ◽  
Floating Tablets ◽  
Drug Concentrations

ABSTRACT Objective: The present study involves preparation and evaluation of floating tablets of ritonavir for improving the drug bioavailability by prolongation of gastric residence time.Ritonavir is an antiretroviral agent used in treatment of HIV and viral diseases has been taken as a model drug in the present investigation because of its low biological half life (3-5h). Moreover it is primarily absorbed from stomach. Materials and Methods: Ritonavir floating tablets were prepared by the dry granulation technique, using guar gum and xanthan gum as polymers, sodium bicarbonate as effervescent agent, PVP as binding agent, Di calcium phosphate as diluents, Crospovidone as swelling agent and magnesium stearate as lubricant. The prepared tablets were evaluated for various physico-chemical parameters. Results: Drug-excipient interaction studies were conducted by FTIR and DSC. The results suggested that there was no incompatibility between the drug and polymers. The prepared tablets were evaluated for their physical characteristics. All the parameters were within the pharmacopoeial limits.  Further, tablets were also studied for their floating properties and in vitro drug release characteristics. The tablets exhibited controlled and prolonged drug release profiles. The developed formulation was found to be stable. Conclusion: The developed floating tablets of ritonavir exhibit prolonged release upto 12 h, and thus may improve bioavailability and minimize fluctuations in plasma drug concentrations. Key words: Ritonavir, floating tablets, gastric residence time, gastroretentive drug delivery system 

Biopharmaceutical and Pharmacodynamic Characteri-stics of Telmisartan Oral Disintegrating Films

2019 ◽  
Vol 12 (2) ◽  
pp. 4489-4496
Author(s):  
Rajesh Kaza ◽  
Sujatha Kumari M ◽  
Kishore Babu M ◽  
Avinash A ◽  
Nagaraju R
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Guar Gum ◽  
Research Work ◽  
Weight Ratio ◽  
Drug Dissolution ◽  
Content Uniformity ◽  
Natural Polymers ◽  
Weight Variation ◽  
Forming Characteristics

This research work was aimed to develop the telmisartan fast dissolving films. Fast dissolving films allow rapid drug dissolution in the oral cavity and thereby bypass the first pass metabolism. Solid dispersions of telmisartan using natural polymers such as hupu gum (HG), guar gum (GG) and xanthan gum (XG) were prepared by kneading technique and the optimized solid dispersion was exploited in the development of rapidly dissolving film. Telmisartan films were prepared by solvent casting method using different grades of HPMC (E5, 50 cps and K4M). Six formulations (FT1-FT6) of telmisartan films were prepared and evaluated for their physical characteristics such as thickness, tensile strength, percentage elongation, weight variation, folding endurance, drug content uniformity and surface pH and gave satisfactory results. The compatibility of the drug in the formulation was confirmed by FTIR and DSC studies. The formulations were subjected to disintegration, in vitro drug release and pharmacodynamic studies on spontaneous hypertensive rats (SHR). Amongst the formulations of FT1-FT6, FT6 was found as best formulation which contains HPMC E5 and telmisartan solid dispersion with guar gum at weight ratio of 1:2 and showed excellent film forming characteristics such as disintegration time at 42 sec and percentage drug release 97.98% within 10 minutes. The optimized film formulation (FT6) showed excellent stability over 45 days when stored at 40°C/60% RH. The pharmacodynamic study in SHR proved that fast dissolving films of telmisartan produced a faster onset of action.    

Development and Evaluation of Bioresponsive Tablets of a Selective COX-2 Inhibitor for Colonic Delivery

2020 ◽  
Vol 10 (1) ◽  
pp. 72-83
Author(s):  
Srushti Tambe ◽  
Namita Desai
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Targeted Delivery ◽  
Guar Gum ◽  
In Vitro Dissolution ◽  
Lag Phase ◽  
Physical Parameters ◽  
Colonic Delivery ◽  
Dissolution Method

Background: We report the effectiveness of a targeted delivery system containing Meloxicam using polysaccharides for the treatment of colorectal cancer. We also propose a novel biorelevant dissolution method to overcome drawbacks of existing dissolution methodologies of polysaccharidebased systems. The proposed method includes a mixture of probiotics cultured under anaerobic conditions in the presence of prebiotic in the in vitro dissolution study to surrogate colonic conditions. Polysaccharide- based system can be simple, safe and effective drug delivery system to target drugs to colon. Methods: Press-coated tablets of Meloxicam were prepared by direct compression using various polysaccharides, such as xanthan gum, guar gum and pectin as coating polysaccharides. Developed tablets were evaluated for physical parameters, lag phase and in vitro drug release. Developed probioticsbased dissolution method was validated and explored for versatility using other polysaccharides. Results: Press-coated tablets of Meloxicam were successfully developed exhibiting targeted delivery to the colon using guar gum as coat and releasing more than 80% of drug in simulated colonic fluid. The developed probiotics based dissolution method may prove to be useful as a bio-relevant and discriminatory method. Conclusion: Developed Meloxicam tablets press-coated with guar gum can be taken orally for treatment or as an adjuvant therapy in colon cancer. Polymers used in this formulation are abundant, nontoxic, biodegradable and inexpensive which make this a a very promising approach for the treatment of different colonic diseases. The proposed biorelevant, animal sparing, probiotics based dissolution medium was found to be versatile to study drug release from other polysaccharide based formulations for colonic delivery.

A Comparative Study of Matrix Tablets Designed by Different Methods

2017 ◽  
Vol 10 (2) ◽  
pp. 3645-3652
Author(s):  
Tulsi Bisht ◽  
Rishishwar Poonam
Keyword(s):  
Drug Release ◽  
Comparative Study ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Once Daily ◽  
Gum Acacia ◽  
Weight Variation ◽  
Evaluation Parameters

The aim of present work was to develop once daily sustained release matrix tablet of aceclofenac by wet granulation technique using natural gums i.e.: gum acacia, guar gum and Xanthan gum. In this present study matrix tablets were prepared using three different methods and a comparative study was done. Aceclofenac sodium being the newer derivative of diclofenac having short biological half life (4hrs.), so it requires more than one dose per day to maintain therapeutic dose. The prepared tablets were evaluated for various parameters like weight variation, hardness, swelling index, friability, percent drug release and various release profile like zero order, first order, Higuchi's, and Koshemeyrs-peppa. All the evaluation parameters met pharmacopoeial specifications and through dissolution studies it was matrix tablets prepared with method 2 shows heighest percent drug release and matrix tablet prepared by method 3 showed lowest percent drug release at the end of 8 hrs. (Shown in fig. 8, comparative release study of all three formulations). Matrix tablet of aceclofenac were successfully prepared and evaluated and it can be concluded that matrix tablet prepared with natural gums showed release rate for a prolonged time and can be of great importance for “once daily” tablet to reduce side effects and toxicity related with NSAIDs.  

scholarly journals Injectable Thermo-Sensitive Chitosan Hydrogel Containing CPT-11-Loaded EGFR-Targeted Graphene Oxide and SLP2 shRNA for Localized Drug/Gene Delivery in Glioblastoma Therapy

2020 ◽  
Vol 21 (19) ◽  
pp. 7111 ◽  
Author(s):  
Yu-Jen Lu ◽  
Yu-Hsiang Lan ◽  
Chi-Cheng Chuang ◽  
Wan-Ting Lu ◽  
Li-Yang Chan ◽  
...  
Keyword(s):  
Graphene Oxide ◽  
Gene Delivery ◽  
Drug Release ◽  
Delivery System ◽  
Targeted Delivery ◽  
Drug Formulation ◽  
Treatment Modalities ◽  
Gene Delivery System ◽  
Optimal Drug

In this study, we aimed to develop a multifunctional drug/gene delivery system for the treatment of glioblastoma multiforme by combining the ligand-mediated active targeting and the pH-triggered drug release features of graphene oxide (GO). Toward this end, we load irinotecan (CPT-11) to cetuximab (CET)-conjugated GO (GO-CET/CPT11) for pH-responsive drug release after endocytosis by epidermal growth factor receptor (EGFR) over-expressed U87 human glioblastoma cells. The ultimate injectable drug/gene delivery system was designed by co-entrapping stomatin-like protein 2 (SLP2) short hairpin RNA (shRNA) and GO-CET/CPT11 in thermosensitive chitosan-g-poly(N-isopropylacrylamide) (CPN) polymer solution, which offers a hydrogel depot for localized, sustained delivery of the therapeutics after the in situ formation of CPN@GO-CET/CPT11@shRNA hydrogel. An optimal drug formulation was achieved by considering both the loading efficiency and loading content of CPT-11 on GO-CET. A sustained and controlled release behavior was found for CPT-11 and shRNA from CPN hydrogel. Confocal microscopy analysis confirmed the intracellular trafficking for the targeted delivery of CPT-11 through interactions of CET with EGFR on the U87 cell surface. The efficient transfection of U87 using SLP2 shRNA was achieved using CPN as a delivery milieu, possibly by the formation of shRNA/CPN polyplex after hydrogel degradation. In vitro cell culture experiments confirmed cell apoptosis induced by CPT-11 released from acid organelles in the cytoplasm by flow cytometry, as well as reduced SLP2 protein expression and inhibited cell migration due to gene silencing. Finally, in vivo therapeutic efficacy was demonstrated using the xenograft of U87 tumor-bearing nude mice through non-invasive intratumoral delivery of CPN@GO-CET/CPT11@shRNA by injection. Overall, we have demonstrated the novelty of this thermosensitive hydrogel to be an excellent depot for the co-delivery of anticancer drugs and siRNA. The in situ forming hydrogel will not only provide extended drug release but also combine the advantages offered by the chitosan-based copolymer structure for siRNA delivery to broaden treatment modalities in cancer therapy.

scholarly journals EXTRACTION, MODIFICATION, AND CHARACTERIZATION OF NATURAL POLYMERS USED IN TRANSDERMAL DRUG DELIVERY SYSTEM: AN UPDATED REVIEW

2020 ◽  
pp. 10-20
Author(s):  
DIPJYOTI BISWAS ◽  
SUDIP DAS ◽  
SOURAV MOHANTO ◽  
SHUBHRAJIT MANTRY
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Drug Delivery ◽  
Biomedical Application ◽  
The Body ◽  
Fixed Dose ◽  
Natural Polymers ◽  
Transdermal Drug Delivery System

The modified/regulated drug delivery system helps to sustain the delivery of the drug for a prolonged period. The modified drug delivery system is primarily aimed at ensuring protection, the effectiveness of the drug, and patient compliance. The transdermal drug delivery system (TDDS) falls within the modified drug delivery system, in which the goal is to deliver the drug at a fixed dose and regulated rate through the skin. Polymers are the backbone of the framework for providing transdermal systems. The polymer should be stable, non-toxic, economical, and provide a sustainable release of the drug. In general, natural polymers used in the TDDS as rate-controlling agents, protective, and stabilizing agents and also used to minimize the frequency of dosing and improve the drug’s effectiveness by localizing at the site of action. Nowadays, manufacturers are likely to use natural polymers due to many issues associated with drug release and side effects with synthetic polymers. Drug release processes from natural polymers include oxidation, diffusion, and swelling. Natural polymers may be used as the basis to achieve predetermined drug distribution throughout the body. The use of natural materials for traditional and modern types of dosage forms are gums, mucilages, resins, and plant waste etc. Thus, the main objective of this review article is to give a brief knowledge about the extraction, modification, characterization, and biomedical application of conventional natural polymers used in the transdermal drug delivery system and their future prospective.

scholarly journals Chitosan and Hydroxy Propyl Methyl Cellulose as a Carrier for Aceclofenac for Prolonged Release

2021 ◽  
pp. 173-182
Author(s):  
R. G. Katedeshmukh ◽  
A. V. Yadav ◽  
J. S. Dhumal ◽  
A. B. Kumbhar ◽  
P. V. Rane ◽  
...  
Keyword(s):  
Drug Release ◽  
Mechanical Strength ◽  
Methyl Cellulose ◽  
Storage Conditions ◽  
Wet Granulation ◽  
Prolonged Release ◽  
Natural Polymers ◽  
Design Expert ◽  
Weight Variation ◽  
Accelerated Stability

Numerous natural polymers either alone or in combination with other polymers were found effective in controlling the drug release. In this study the attempts were made to combine chitosan (degree of deacetylation 84.14 %) and as hydroxylpropyl methylcellulose (HPMC K 15M) to retard the release of aceclofenac in tablet formulation. The tablets were prepared by wet granulation and evaluated for pre and post- compression parameters. All the pre-compression parameters were found within the limit.  Hardness and friability values were found in the range of 4.30-4.89 kg/cm2 and 0.1-0.6% respectively. These results proved the good mechanical strength of the formulations.  The drug content was found in the range of 97.56 – 99.10 %.  Weight variation was found within the official limit. The percent drug release and swelling index was found to be dependent on the concentration of polymer. With increasing the concentration of both the polymers the swelling index was increased and drug release decrease. Highest concentration of both the polymers was found to retard the drug release up to 8 h.  The effect of Chitosan and HPMC on drug release was evaluated by design expert software to achieve the optimized formulation. The response of the drug release after 4h was considered to check the drug release. It was found that the enhanced concentration of both the polymers had negative effective on the drug release. The formulation containing highest concentration of the chitosan and HPMC was found be fit in the limits of optimized formulations. The optimized formulation was found to be stable at accelerated stability storage conditions.

scholarly journals Formulation of Metformin Sustained Release Tablet Using Natural Polymer

2021 ◽  
Vol 11 (2) ◽  
pp. 31-37
Author(s):  
Mehak Siddiqui ◽  
L. K. Omray ◽  
Pushpendra Soni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Absolute Bioavailability ◽  
Dissolution Time ◽  
Content Uniformity ◽  
Weight Variation

The overall objective of the present work was to develop an oral sustained-release (SR) Metformin tablet that is prepared by the direct compression method by using hydrophilic hydroxyl propyl methyl cellulose (HPMC) and Guar gum polymer alone as well as in combination at different concentrations. Metformin is a biguanide that has a relatively short plasma half-life. It has low absolute bioavailability. All the properties were evaluated for thickness, weight variation, hardness and drug content uniformity and in vitro drug release. The mean dissolution time is used to characterize the drug release rate from a dosage form that indicates the drug release-retarding efficiency of the polymer. The hydrophilic matrix of HPMC alone could not control the Metformin release effectively for 12 h but when combined with Guar gum, it could slow down the release of drug and, thus, can be successfully employed for formulating Sustain Release matrix tablets. Keywords: Guar gum, hydroxylpropylmethylcellulose, matrix tablets, release kinetics,

scholarly journals APPLICABILITY OF NANOPARTICLES-HYDROGEL COMPOSITE IN TREATING PERIODONTAL DISEASES AND BEYOND

2017 ◽  
Vol 10 (2) ◽  
pp. 65 ◽  
Author(s):  
Nafiu Aminu ◽  
Seok Ming Toh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Periodontal Disease ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Periodontal Diseases ◽  
Delivery Systems ◽  
Natural Polymers ◽  
Hydrogel Composite ◽  
Multiple Drugs

Nanoparticles-Hydrogel Composite (nanogels) have yielded a surge in the design and development of novel drug delivery systems for the treatment of many ailments, including periodontal disease. The recent innovations in nanotechnological drug carrier systems seem promising, as it provides a means to improve the bioavailability of poorly soluble drugs, formulations of controlled and targeted drug delivery systems, drug release control base on the stimuli response, among others. Several polymeric nanoparticles-hydrogel co-formulations have been investigated during the last few years, mostly using synthetic & natural polymers. Some of the results and rewards achieved from these novel approaches are the use of bioadhesive polymers to achieve prolong drug release, the increment of intra-pocket drug penetration, the enhancement of mechanical properties using chemical crosslinkers and the possibility of loading multiple drugs in a unit delivery system.  Furthermore, these nanotechnological advances have also shown that nanoparticles (NPs) possess great potential as drug carriers in periodontal disease treatment. The future utilization of these advantages will significantly improve dental care. The co-formulation of nanoparticles-hydrogel composite will yield additional benefits that are much greater than ordinary NPs or hydrogels in delivering of drug into the periodontal pockets. The aim of this review article is to summarises updates on the current and future nanotechnological approaches that are being investigated for the treatment of periodontitis, with particular attention to the nanogels, and to identify arenas which its exploration might lead to the development of an effective intra-pocket drug delivery systems for the treatment of periodontal diseases. The review also provided brief applications of nanogels in the management of other diseases.Keywords: Nanocomposite, Hydrogels, Nanoparticles, Nanogels, Periodontal intra-pocket drug delivery system, Nanotechnological approaches.

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