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Fundamentals Of Analytical Chemistry

The excellent therapeutic potential of a variety of phytochemicals in different diseases has been proven by extensive studies throughout history. However, most phytochemicals are characterized by a high molecular weight, poor aqueous solubility, limited gastrointestinal permeability, extensive pre-systemic metabolism, and poor stability in the harsh gastrointestinal milieu. Therefore, loading of these phytochemicals in biodegradable and biocompatible nanoparticles (NPs) might be an effective approach to improve their bioactivity. Different nanocarrier systems have been developed in recent decades to deliver phytochemicals. Among them, NPs based on chitosan (CS) (CS-NPs), a mucoadhesive, non-toxic, and biodegradable polysaccharide, are considered the best nanoplatform for the oral delivery of phytochemicals. This review highlights the oral delivery of natural products, i.e., phytochemicals, encapsulated in NPs prepared from a natural polymer, i.e., CS, for improved bioavailability and bioactivity. The unique properties of CS for oral delivery such as its mucoadhesiveness, non-toxicity, excellent stability in the harsh environment of the GIT, good solubility in slightly acidic and alkaline conditions, and ability to enhance intestinal permeability are discussed first, and then the outcomes of various phytochemical-loaded CS-NPs after oral administration are discussed in detail. Furthermore, different challenges associated with the oral delivery of phytochemicals with CS-NPs and future directions are also discussed.

Recent Advancement in Chitosan-Based Nanoparticles for Improved Oral Bioavailability and Bioactivity of Phytochemicals: Challenges and Perspectives.

Trans-ferulic acid (FA) is a derivative of 4-hydroxycinnamic acid, which is found in many food products, fruits and beverages. It has scientifically proven antioxidant, anti-inflammatory and antibacterial properties. However, its low ability to permeate through biological barriers (e.g., the blood–brain barrier, BBB), its low bioavailability and its fast elimination from the gastrointestinal tract after oral administration limit its clinical use, e.g., for the treatment of neurodegenerative diseases, such as Alzheimer’s disease. Therefore, new nanotechnological approaches are developed in order to regulate intracellular transport of ferulic acid. The objective of this review is to summarize the last decade’s research on biological properties of ferulic acid and innovative ways of its delivery, supporting pharmacological therapy.

Recent Advances in Biological Activity, New Formulations and Prodrugs of Ferulic Acid

Nature has provided therapeutic substances for millennia, with many valuable medications derived from plant sources. Multitarget drugs become essential in the management of various disorders, including hepatic disorders, neurological disorders, diabetes, and carcinomas. Ferulic acid is a significant potential therapeutic agent, which is easily available at low cost, possesses a low toxicity profile, and has minimum side effects. Ferulic acid exhibits various therapeutic actions by modulation of various signal transduction pathways such as Nrf2, p38, and mTOR. The actions exhibited by ferulic acid include anti-apoptosis, antioxidant, anti-inflammatory, antidiabetic, anticarcinogenic, hepatoprotection, cardioprotection, activation of transcriptional factors, expression of genes, regulation of enzyme activity, and neuroprotection, which further help in treating various pathophysiological conditions such as cancer, skin diseases, brain disorders, diabetes, Parkinson's disease, Alzheimer's disease, hypoxia, hepatic disorders, H1N1 flu, and viral infections. The current review focuses on the significance of natural products as sources of multitarget compounds, and a primary focus has been made on ferulic acid and its mechanism, role, and protective action in various ailments. 

Natural Products as Sources of Multitarget Compounds: Advances in the Development of Ferulic Acid as Multitarget Therapeutic

Oral ingestion is most convenient and commonly employed route of drug delivery due to its ease of administration, least aseptic and flexibility in the design of dosage form. The objective of the study was to explore the necessity, advantages and various techniques of extended release matrix tablet to get a constant drug delivery rate and reproducible kinetics for advance delivery. Different types of extended release matrix tablet have been explained briefly along with the various formulation which mainly by wet granulation or direct compression method or by dispersion of solid particle within a porous matrix formed by using different polymers. Matrix controls the free rate of drug. Matrix tablets can be formulated by either direct compression or wet granulation method by using a variety of hydrophilic or hydrophobic polymers. The extended release matrix tablets can assure better patient compliance through reduction in total dose and dosage regimen, which can be great help to treat chronic diseases. This review highlights the types of matrices, mechanisms involved and evaluation studies.
                    

Peer Review History: 
Received 20 December 2018;   Revised 28 December; Accepted 31 December, Available online 15 January 2019
Academic Editor: 
Dr. Iman Muhammad Higazy, National Research Center, Egypt, imane.higazy@hotmail.com
UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency.
Received file:  Reviewer's Comments:
Average Peer review marks at initial stage: 5.5/10
Average Peer review marks at publication stage: 7.5/10
Reviewer(s) detail:
Dr. Sally A. El-Zahaby, Pharos University in Alexandria, Egypt, sally.elzahaby@yahoo.com
Dr. Maha Khalifa Ahmed Khalifa, Al-Azhar Universit - Cairo, Egypt, mahakhalifa.ahmed@hotmail.com
Similar Articles:
FORMULATION AND EVALUATION OF FINASTERIDE SUSTAINED-RELEASE MATRIX TABLETS USING DIFFERENT RATE CONTROLLING POLYMERS 
QUALITY ASSESSMENT OF DIFFERENT BRANDS OF PARACETAMOL TABLETS IN YEMENI MARKET
DEVELOPMENT AND CHARACTERIZATION OF DIRECT COMPRESSED MATRIX MINI TABLETS OF NAPROXEN SODIUM 
FORMULATION AND EVALUATION OF COLON TARGETED MATRIX TABLETS CONTAINING EXTRACT OF SOLENOSTEMMA ARGEL (HARGEL)

http://ujpr.org/index.php/journal/article/download/222/152

A comprehensive review on sustained release matrix tablets: a promising dosage form

Use of combined nanocarrier system based on chitosan nanoparticles and phospholipids complex for improved delivery of ferulic acid.

Three-dimensional printing (3DP) technology is an innovative tool used in manufacturing medical devices, producing alloys, replacing biological tissues, producing customized dosage forms and so on. Stereolithography (SLA), a 3D printing technique, is very rapid and highly accurate and produces finished products of uniform quality. 3D formulations have been optimized with a perfect tool of artificial intelligence learning techniques. Complex designs/shapes can be fabricated through SLA using the photopolymerization principle. Different 3DP technologies are introduced and the most promising of these, SLA, and its commercial applications, are focused on. The high speed and effectiveness of SLA are highlighted. The working principle of SLA, the materials used and applications of the technique in a wide range of different sectors are highlighted in this review. An innovative idea of 3D printing customized pharmaceutical dosage forms is also presented. SLA compromises several advantages over other methods, such as cost effectiveness, controlled integrity of materials and greater speed. The development of SLA has allowed the development of printed pharmaceutical devices. Considering the present trends, it is expected that SLA will be used along with conventional methods of manufacturing of 3D model. This 3D printing technology may be utilized as a novel tool for delivering drugs on demand. This review will be useful for researchers working on 3D printing technologies.

Stereolithography 3D printing technology in pharmaceuticals: a review.

Objective: The objective of the present study was to formulate the gastro-retentive floating tablets containing Ibuprofen, which would remain in stomach and/or upper part of GIT for prolonged period of time. Floating systems have low bulk density so that they can float on the gastric juice in the stomach. Ibuprofen is an anti inflammatory drug.  
Methods: On trial and error basis formulation design was done. Four different batches of floating tablets of Ibuprofen were prepared using HPMC, Xanthan gum, and gas generating agent sodium bicarbonate and citric acid. The tablets were characterized for the pre and post compression parameters such as friability, hardness, thickness, drug content, weight variation, in-vitro buoyancy studies and 13 hrs in-vitro drug release studies and the results were within the limits.
Results: There was no interaction found in between drug and other ingredients. Maximum release was shown by formulation of batch F4 (47.38%), and minimum by the formulations of batch F2 (34.46%) in the duration of 13 hrs.
Conclusion: From the results obtained, it was concluded that the optimized formulation F4 desired drug release properties and floating behavior.

    
Peer Review History: 
Received 13 June 2018;   Revised 26 August; Accepted 3 September, Available online 15 September 2018
UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency.
Received file:  Reviewer's Comments:
Average Peer review marks at initial stage: 2/10
Average Peer review marks at publication stage: 7/10
Reviewer(s) detail:
Dr. Heba M. Abd El-Azim, Damanhour University, Egypt, h_m_abdelazim@hotmail.com
Dr. Sally A. El-Zahaby, Pharos University in Alexandria, Egypt, sally.elzahaby@yahoo.com
Similar Articles:
DEVELOPMENT AND EVALUATION OF RITONAVIR HOLLOW MICROBALLOONS FOR FLOATING DRUG DELIVERY 
DEVELOPMENT AND EVALUATION OF IN SITU GELLING GASTRORETENTIVE FORMULATIONS OF MELOXICAM 
This article has been cited by:
Sachin Sarashetti, Vikas Jain, Gowda D V, Pooja Mallya, & Satish Babu. (2020). Recent developments in orally disintegrating mini tablets. International Journal of Research in Pharmaceutical Sciences, 11(3), 3606-3612. Pubmed

/pdf/formulation-and-evaluation-of-ibuprofen-gastro-retentive-3v9l23npew.pdf

Formulation and evaluation of ibuprofen gastro-retentive floating tablets

Although there are rapid developments in molecular science and synthetic chemistry for investigation of many essential drug molecules, poor solubility and bioavailability issues are major constraint in the design of more efficient formulations. This research study focuses on the enhancement of solubility and development of the bucco-adhesive drug delivery system of bosentan using Soluplus® (polyvinyl-caprolactam-polyvinyl-acetate-polyethylene glycol graft co-polymer) as a carrier. A 32-factorial design was implemented to develop bucco-adhesive tablets using hydroxypropyl methyl cellulose (HPMC) K100 LV (X1) and Carbopol 934 P (X2) as independent variables at various levels whereas t50%(Y1) (time required to release 50% of drug), Rel4h (Y2) (percentage of the drug release in 4 h) and bio-adhesive strength (Y3) were considered as set response parameters. The positive effect of the surface response quadratic model demonstrated the change in the already set dependent variables of t50%, Rel4h and bio-adhesive strength. The FT-IR study confirmed the suitability of all the components used in the design of formulation. DSC and XRD study have confirmed the encapsulation of bosentan in the Soluplus® carrier and amorphous form of bosentan, respectively. Overall, 6.832-fold increase in solubility was observed for bosentan-solid dispersion. High-water uptake and swelling of bucco-adhesive tablets (containing bosentan-solid dispersion) was observed due to presence of the highly hydrophilic-Soluplus®. Rel4hwas found to be 97.86 ± 0.57% for optimized formulation (F4) and was decreased with increasing polymer content. The values of t50% were found to be enhanced from 1.11 to 2.32 h at the lower to higher levels of both the polymers respectively.

An effort to augment solubility and efficiency of the oral bosentan-bucco-adhesive drug delivery system using graft co-polymer as the carrier

Hydrochlorothiazide (HTZ) is a first-line drug used in the treatment of hypertension suffered from low oral bioavailability due to poor aqueous solubility and permeability. Hence, lyophilized egg white protein-based solid dispersion (HTZ-EWP SD) was developed to explore its feasibility as a solid dispersion carrier for enhanced aqueous solubility and permeability of HTZ. The HTZ-EWP SD was prepared using the kneading method. HTZ-EWP SD was characterized using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FT-IR), powder X-ray diffractometer (PXRD), solubility, in vitro dissolution, and ex vivo permeation studies. The physico-chemical evaluation suggested the formation of the solid dispersion. Optimized HTZ-EWP SD4 drastically enhanced (~32-fold) aqueous solubility (~16.12 ± 0.08 mg/mL) over to pure HTZ (~ 0.51 ± 0.03 mg/mL). The dissolution study in phosphate buffer media (pH 6.8) revealed that HTZ-EWP SD4 significantly enhanced the release rate of HTZ (~ 87 %) over to HTZ (~ 25 %). The permeation rate of HTZ from optimized HTZ-EWP SD4 was enhanced significantly (~ 84 %) compared to pure HTZ (~ 24 %). Optimized HTZ-EWP-SD4 enhanced the rate of HTZ dissolution (~ 86 %) in FeSSIF (fed state simulated intestinal fluid), compared to a low dissolution rate (~ 72 %) in FaSSIF (fasted state simulated intestinal fluid) state after 2-h study. Obtained results conclude that lyophilized egg white protein can be utilized as an alternative solid dispersion carrier for enhancing the solubility and permeability of HTZ.

Egg White Protein Carrier-Assisted Development of Solid Dispersion for Improved Aqueous Solubility and Permeability of Poorly Water Soluble Hydrochlorothiazide

Shirish P. Jain

Papers

Use of combined nanocarrier system based on chitosan nanoparticles and phospholipids complex for improved delivery of ferulic acid.

Stereolithography 3D printing technology in pharmaceuticals: a review.

Formulation and evaluation of ibuprofen gastro-retentive floating tablets

An effort to augment solubility and efficiency of the oral bosentan-bucco-adhesive drug delivery system using graft co-polymer as the carrier

Egg White Protein Carrier-Assisted Development of Solid Dispersion for Improved Aqueous Solubility and Permeability of Poorly Water Soluble Hydrochlorothiazide