New insights into the effects of porosity, pore length, pore shape and pore alignment on drug release from extrusion-based additive manufactured pharmaceuticals

Melanoma is the most dangerous type of skin cancer in which mostly damaged unpaired DNA starts mutating abnormally and staged an unprecedented proliferation of epithelial skin to form a malignant tumor. In epidemics of skin, pigment-forming melanocytes of basal cells start depleting and form uneven black or brown moles. Melanoma can further spread all over the body parts and could become hard to detect. In USA Melanoma kills an estimated 10,130 people annually. This challenge can be succumbed by using the certain anti-cancer drug. In this study design, cyclophosphamide were used as a model drug. But it has own limitation like mild to moderate use may cause severe cytopenia, hemorrhagic cystitis, neutropenia, alopecia and GI disturbance. This is a promising challenge, which is caused due to the increasing in plasma drug concentration above therapeutic level and due to no rate limiting steps involved in formulation design. In this study, we tried to modify drug release up to threefold and extended the release of drug by preparing and designing niosome based topical gel. In the presence of Dichloromethane, Span60 and cholesterol, the initial niosomes were prepared using vacuum evaporator. The optimum percentage drug entrapment efficacy, zeta potential, particle size was found to be 72.16%, 6.19mV, 1.67µm.Prepared niosomes were further characterized using TEM analyzer. The optimum batch of niosomes was selected and incorporated into topical gel preparation. Cold inversion method and Poloxamer -188 and HPMC as core polymers, were used to prepare cyclophosphamide niosome based topical gel. The formula was designed using Design expert 7.0.0 software and Box-Behnken Design model was selected. Almost all the evaluation parameters were studied and reported. The MTT shows good % cell growth inhibition by prepared niosome based gel against of A375 cell line. The drug release was extended up to 20th hours. Further as per ICH Q1A (R2), guideline 6 month stability studies were performed. The results were satisfactory and indicating a good formulation approach design was achieved for Melanoma treatment.

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Effects of release modifier on Carvedilol release from Kollidon SR based matrix

International Current Pharmaceutical Journal ◽

10.3329/icpj.v1i8.11095 ◽

2012 ◽

Vol 1 (8) ◽

pp. 186 ◽

Cited By ~ 1

Author(s):

Urmi Das ◽

Mohammad Salim Hossain

Keyword(s):

Drug Release ◽

Sustained Release ◽

Microcrystalline Cellulose ◽

Matrix Tablets ◽

Dissolution Time ◽

Release Mechanism ◽

Matrix Tablet ◽

Weight Variation ◽

The Matrix ◽

Tablet Formulations

Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a> International Current Pharmaceutical Journal 2012, 1(8): 186-192

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Modeling of Drug Release from Polymeric Delivery Systems?A Review;

Critical Reviews in Therapeutic Drug Carrier Systems ◽

10.1615/critrevtherdrugcarriersyst.v21.i5.10 ◽

2004 ◽

Vol 21 (5) ◽

pp. 345-386 ◽

Cited By ~ 71

Author(s):

Stephanie T. Lopina ◽

Deenu G. Kanjickal

Keyword(s):

Drug Release ◽

Delivery Systems ◽

Polymeric Delivery

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The Improvement of Paclitaxel Cytotoxicity using Nanocellulose based Nature Resources

Journal of Engineering and Scientific Research ◽

10.23960/jesr.v1i1.3 ◽

2019 ◽

Vol 1 (1) ◽

pp. 7

Author(s):

R Nahrowi ◽

A Setiawan ◽

Noviany Noviany ◽

I Sukmana ◽

S D Yuwono

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Natural Resources ◽

Cell Viability ◽

Cancer Cells ◽

Drug Delivery System ◽

Target Cell ◽

Mitotic Cycle ◽

Potential Sources ◽

Local Accumulation

Paclitaxel is one of the cancer drugs that often used. These drug kills cancer cells byinhibiting mitotic cycle. The efficiency of paclitaxel is increased by the use ofnanomaterials as a carrier of paclitaxel. Nanomaterials can enhance encapsulationefficiency, improve the drug release to the target cell following nanomaterialdegradation, and improve local accumulation of drug in the cell through endocytosisreceptor. Nanomaterial that often used forencapsulation of paclitaxel is a polymerderived from natural resources such as cellulose. The advantages of cellulose as acarrier of paclitaxel are nontoxic, biodegradable, and very abundant from varioussources. One of the potential sources of cellulose for drug delivery system is cassavabaggase.Keywords: Paclitaxel, encapsulation, cell viability, nanocellulose

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Acyclovir Loaded Solid Lipid Nanoparticle Based Cream: A Novel Drug Delivery System

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v7i1.8917 ◽

2017 ◽

Vol 7 (1) ◽

Author(s):

EL- Assal I. A. ◽

Retnowati .

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Antiviral Agent ◽

Study Drug ◽

Particle Size Analysis ◽

Stability Study ◽

Size Analysis ◽

Solid Lipid ◽

Dermal Delivery

Objective of the present investigation was enthused by the possibility to develop solid lipid nanoparticles (SLNs) of hydrophilic drug acyclovir. Also study vitro and vivo drug delivery. Methods: Drug loaded SLNs (ACV-SLNs) were prepared by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state with formula optimization study (Different lipid concentration, drug loaded, homogenization / stirring speed and compritol 888ATO: drug ratio). ACV - SLN incorporated in cream base. The pH was evaluated and rheological study. Drug release was evaluated and compared with simple cream- drug, ACV – SLN with compritol 888ATO and marketed cream. The potential of SLN as the carrier for dermal delivery was studied. Results: Particle size analysis of SLNs prove small, smooth, spherical shape particle ranged from 150 to 200 nm for unloaded and from 330 to 444 nm for ACV loaded particles. The EE% for optimal formula is 72% with suitable pH for skin application. Rheological behavior is shear thinning and thixotropic. Release study proved controlled drug release for SLNs especially in formula containing compritol88 ATO. Stability study emphasized an insignificant change in SLNs properties over 6 month. In-vivo study showed significantly higher accumulation of ACV in stratum corneum, dermal layer, and receptor compartment compared with blank skin. Conclusion: AVC-loaded SLNs might be beneficial in controlling drug release, stable and improving dermal delivery of antiviral agent(s).

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Formulation and Optimization of Immediate Release Pellets of Antiplatelet Drugs Using Design of Experimentation

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v7i04.10648 ◽

2017 ◽

Vol 7 (04) ◽

Author(s):

Deshkar S. S. ◽

Pore A. R.

Keyword(s):

Platelet Aggregation ◽

Drug Release ◽

Peripheral Arterial Disease ◽

Tissue Injury ◽

Immediate Release ◽

Arterial Disease ◽

Fixed Dose ◽

Disintegration Time ◽

Peripheral Arterial ◽

Pvp K30

Platelets play an important role in hemostasis during tissue injury, which blocks the defect and terminates blood loss. Platelet aggregation inhibitors are widely used in treatment of cardiovascular disorders and Peripheral arterial disease. Clopidogrel bisulphate and Cilostazol, are FDA approved BCS class II drugs, used in treatment of Platelet aggregation, peripheral arterial disease and intermittent claudication. The aim of the present study was to develop an immediate release pellets for combination of Clopidogrel bisulphate and Cilostazol using extrusion spheronization technique. The effects of spheronization speed(X1) and binder concentration (PVP K30) (X2), on size of pellets, disintegration time and drug release were studied using 32 full factorial design. The surface response and counter plot were drawn to facilitate an understanding of the contribution of the variables and their interaction. From the results, speed of spheronization of 1100 rpm and 5% concentration of PVP K30, were selected. In vitro drug release studies revealed more than 80% of clopidogrel bisulphate release and more than 75% of cilostazol release within 30 min of dissolution which complied with the pharmacopoeal limits. Film coated pellets did not show significant change in the drug release. DSC and FTIR studies revealed no interaction of drugs and excipient during pellet formulation. The pellet formulations of clopidogrel and cilostazol were found to be stable when stored at 40ºC±2ºC/ 75%RH±5%RH for 2 months. Conclusively, clopidogrel bisulphate and cilostazol pellet fixed dose combination could be successfully developed by design of experimentation and complied with pharmacopoeal limits.

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Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v7i04.10647 ◽

2017 ◽

Vol 7 (04) ◽

Author(s):

ShirishaG. Suddala ◽

S. K. Sahoo ◽

M. R. Yamsani

Keyword(s):

Rheumatoid Arthritis ◽

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Lag Time ◽

Oral Dosage ◽

Lag Phase ◽

Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

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Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v6i1.8883 ◽

2016 ◽

Vol 6 (1) ◽

Author(s):

Anamika Saxena Saxena ◽

Santosh Kitawat ◽

Kalpesh Gaur ◽

Virendra Singh

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery Systems ◽

Entrapment Efficiency ◽

Repeated Administration ◽

Alginate Beads ◽

Delivery Systems ◽

Sem Analysis ◽

Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

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