scholarly journals Experimental Design: Approaches and Applications in Development of Pharmaceutical Drug Delivery System

2021 ◽  
Vol 11 (4-S) ◽  
pp. 154-161
Author(s):  
Vinanti Supare ◽  
Kamlesh Wadher ◽  
Milind Umekar
Keyword(s):  
Drug Delivery ◽  
Experimental Design ◽  
Delivery System ◽  
Pharmaceutical Formulations ◽  
System Optimization ◽  
Optimization Techniques ◽  
Experimental Designs ◽  
Screening Designs ◽  
Minimum Number ◽  
Analytical Tools

Conventionally, all the delivery systems have been prepared by methodology of trial and error concept by manipulating one variable at a Time, but attainment of optimal formulation is not achievable. The systematic approach Design of Experiments (DoE) enables researchers to provide appropriate outline to develop a best optimized delivery system. Optimization techniques using DoE helps to provide effective and economical analytical tools to find the perfect solution for a particular problem. In screening designs, there is large number of screening factors in minimum number of experiments and beneficial to minimize the variables in a desired size therefore further experimentation may be performed easily by using these variables. Experimental designs and optimization techniques are the tools which are systematically used to categorize various types of problems that may influence development of pharmaceutical delivery system. Use of experimental design is the best approach to the screening and optimization of experimental factors. In the present review article we have focused on application of practically applicable experimental designs and optimization techniques for the development of quality and efficacious of pharmaceutical formulations such as, nanoparticles, Phytosomes, microspheres, liposomes, micells, films, nanostructured lipid carriers and tablets and which type of factors to be considered while optimization are also discussed. Keywords: Experimental design, Optimization, Applications, Drug delivery, Phytosomes, Nano delivery System.

scholarly journals Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 544
Author(s):  
Miao Wang ◽  
Sung-Kyun You ◽  
Hong-Ki Lee ◽  
Min-Gu Han ◽  
Hyeon-Min Lee ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Anticancer Agents ◽  
Lipid Membrane ◽  
Ex Vivo ◽  
System Optimization ◽  
Raw Material ◽  
Phospholipid Complex ◽  
Low Solubility

Docetaxel (DTX) has clinical efficacy in the treatment of breast cancer, but it is difficult to develop a product for oral administration, due to low solubility and permeability. This study focused on preparing a self-microemulsifying drug delivery system (SME) loaded with DTX-phospholipid complex (DTX@PLC), to improve the dissolution and gastrointestinal (GI) permeability of DTX. A dual technique combining the phospholipid complexation and SME formulation described as improving upon the disadvantages of DTX has been proposed. We hypothesized that the complexation of DTX with phospholipids can improve the lipophilicity of DTX, thereby increasing the affinity of the drug to the cell lipid membrane, and simultaneously improving permeability through the GI barrier. Meanwhile, DTX@PLC-loaded SME (DTX@PLC-SME) increases the dissolution and surface area of DTX by forming a microemulsion in the intestinal fluid, providing sufficient opportunity for the drug to contact the GI membrane. First, we prepared DTX@PLC-SME by combining dual technologies, which are advantages for oral absorption. Next, we optimized DTX@PLC-SME with nanosized droplets (117.1 nm), low precipitation (8.9%), and high solubility (33.0 mg/g), which formed a homogeneous microemulsion in the aqueous phase. Dissolution and cellular uptake studies demonstrated that DTX@PLC-SME showed 5.6-fold higher dissolution and 2.3-fold higher DTX uptake in Caco-2 cells than raw material. In addition, an ex vivo gut sac study confirmed that DTX@PLC-SME improved GI permeability of DTX by 2.6-fold compared to raw material. These results suggested that DTX@PLC-SME can significantly overcome the disadvantages of anticancer agents, such as low solubility and permeability.

scholarly journals Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
System Optimization ◽  
Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

scholarly journals Nanostructured Lipid Carriers: A Groundbreaking Approach for Transdermal Drug Delivery

2020 ◽  
Vol 10 (2) ◽  
pp. 150-165 ◽  
Author(s):  
Iti Chauhan ◽  
Mohd Yasir ◽  
Madhu Verma ◽  
Alok Pratap Singh
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
First Generation ◽  
Drug Loading ◽  
Scale Up ◽  
Pharmaceutical Formulations ◽  
Nanostructured Lipid Carriers ◽  
Beneficial Effects ◽  
Skin Targeting

Nanostructured lipid carriers (NLCs) are novel pharmaceutical formulations which are composed of physiological and biocompatible lipids, surfactants and co-surfactants. Over time, as a second generation lipid nanocarrier NLC has emerged as an alternative to first generation nanoparticles. This review article highlights the structure, composition, various formulation methodologies, and characterization of NLCs which are prerequisites in formulating a stable drug delivery system. NLCs hold an eminent potential in pharmaceuticals and cosmetics market because of extensive beneficial effects like skin hydration, occlusion, enhanced bioavailability, and skin targeting. This article aims to evoke an interest in the current state of art NLC by discussing their promising assistance in topical drug delivery system. The key attributes of NLC that make them a promising drug delivery system are ease of preparation, biocompatibility, the feasibility of scale up, non-toxicity, improved drug loading, and stability.

OPTIMIZATION TECHNIQUES IN DESIGNING PHARMACEUTICAL FORMULATIONS

2021 ◽  
pp. 38-40
Author(s):  
Pusukuri Navya ◽  
Priyarini k ◽  
Tejaswi k ◽  
Prasanthi D
Keyword(s):  
Factorial Design ◽  
Optimization Design ◽  
Fractional Factorial Design ◽  
Pharmaceutical Formulations ◽  
Optimization Techniques ◽  
Fractional Factorial ◽  
Experimental Designs ◽  
Sequential Optimization ◽  
Box Behnken Design ◽  
Central Composite

This review determines various optimization techniques which are used commercially for pharmaceutical formulations. A glance on the terminology used in optimization, about the software which is used for design of experiments and information regarding optimization parameters.In this various experimental designs are listed such as Factorial design, fractional factorial design,mixture design, star design, Plackett-Burmann design,Central composite design, Box-Behnken design, Taguchi design, D-Optimal design,sequential optimization design etc.In this it describes about the future scope of the optimization techniques and also various types of experimental designs used for various research works were listed. Thus optimization techniques plays key role in the formulation of various pharmaceutical formulations which brings prots and save time for pharmaceutical industry.

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