Volume 12, Issue 4, Oct-Dec 2020

Volume 12

October-December 2020

Microspheres and microcapsules: A review of manufacturing techniques ‎for pharmaceutical ‎industries‎

Paroma Arefin, Md Shehan Habib, Nazim Uddin Ahmed, Md Abdurrahim, Md Ibrahim, Sreebash Chandra Bhattacharjee, Dipankar Chakraborty, Sumon Das, Debabrata Karmakar, Dip Bhowmik, Shirmin Islam, Md Saidul Arefin

Abstract:
Microencapsulation is a technique by which a layer of polymer or any other coating material is provided to small particles of solid or liquid substances. Microspheres are used for a number of purposes like in food industries, food preservation, drug formulations, and so on. Depending on purposes of use and production requirements, different methods are used. In case of drug formulations, microencapsules or microspheres facilitate masking bitter or undesirable taste of a substance, long duration of action, site-specific release, separation of incompatible substances, and protection against moisture degradation or oxidation, modifying elements’ physical characteristics. Microspheres can be produced in various ways. These methods can be categorized as physical, physicochemical and chemical methods. They can also be categorized as chemical and mechanical processes. Researchers have always explored different ways of microsphere production to discover new applications. In this review paper, we have highlighted different methods used for the microsphere and microcapsule preparation. Spray drying or congealing, coacervation and solvent evaporation techniques are most commonly used for drug formulation preparation. This research can be a guideline to find out the most suitable method of microsphere preparation depending on the desired output.

Keywords: Microsphere, Microcapsule, Solvent Evaporation, Spray Drying, Coacervation.

Overview on ligands for the targeting in treatment of glioblastoma

Sachin D Chaudhari, Pankaj P Nerkar

Abstract:
Glioblastoma is a grade IV malignant primary central nervous system tumor with ‎poor prognosis. Radiotherapy chemotherapy, surgical resection are the current ‎therapies use for the management of GBM, but it can also cause dangerous side ‎effects hence targeted therapies are in development. In targeted therapies, ‎receptor targeted drug delivery is one of the most successful strategy. A receptor ‎which are more express over the cancerous tissue or blood brain barrier that can ‎be easily targeted and it is advantage to differentiate cancerous tissue and normal ‎tissue. We summaries receptor targeted therapies and reagent used for ‎conjugating or coupling ligand to drug. ‎

Keywords: Glioblastoma, Single Receptor Targeting, Dual Receptor Targeting, Transferrin, Lactoferrin, Folic Acid.

Fast dissolving tablets as an ideal system for immediate drug delivery: A review

Maria John, Fels Saju

Abstract:
Fast dissolving tablets (FDTs) are the formulations that dissolve within a few ‎seconds when coming in contact with saliva. Superdisintegrants like ‎Microcrystalline Cellulose, Cross-povidone, Cross Carmellose, and Sodium Starch ‎Glycolate cause the easy breakup of the tablets. Direct compression, moulding, ‎and lyophilisation are the common techniques used for the production of the ‎tablets. Fast dissolution in the oral cavity makes a drug more suitable for geriatric ‎and pediatric patients. It is most effective for those drugs which need quick onset ‎of action. Also, it provides the benefits of both solid and liquid dosage forms. ‎

Keywords: Fast Dissolving Tablet, Super Disintegrants, Oral Dosage Form.

Total phenolic contents, DPPH ‎radical scavenging and β-carotene ‎bleaching activities of ethyl acetate ‎extract from Saccocalyx ‎satureioides Coss and Dur

Soulaf Mehlous, Fatima Benchikh, Hassiba Benabdallah, Karima Loucif, Chahrazed Kaoudoune, Hocine Laouer, Smain Amira

Abstract:
Saccocalyx satureioides Coss and Dur, an endemic species of Algeria, has attracted a great attention due to its traditional medicinal usage for gastric disorders and spasms. The purpose of this study was to estimate the total phenolics and flavonoids content, and the in vitro antioxidant capacity of the ethyl acetate extract (EAE) from Saccocalyx satureioides Coss and Dur aerial part. Folin-Ciocalteu’s reagent and Aluminum chloride (AlCl₃) were used to quantify the total polyphenols and flavonoids content, respectively. However, DPPH (1,1-diphenyl-2-picrylhydrazyl) and β-carotene bleaching method were applied to assess the in vitro antioxidant activity. Total phenolic and flavonoid content in the extract were 317.55 ±1.38 mg gallic acid equivalent/g of dry extract (GAE/g) and 40.38 ± 0.88 mg quercetin equivalent / g of dry extract (QE/g), respectively. The EAE extract has an important capacity to scavenge the free radical DPPH with an IC₅₀ of 0.02±0.00048mg/ml. In addition, it was powerfully able to inhibit the lipid peroxidation with a percentage of 71.59± 0.53%. The results of the present study may prove that the medicinal plants are a good resource of natural antioxidants.

Keywords: Saccocalyx satureioides, Ethyl Acetate Extract, Polyphenols, Flavonoids, Antioxidant Activity.

Bioavailability enhancement and ‎dissolution rate of poor water ‎soluble drug by solid dispersion ‎technique

Ajay Kumar Shukla, Ram Singh Bishnoi, Manish Kumar, C P Jain, Ritesh Tiwari, Ritu Jain

Abstract:
The aim of the present study was to increase solubility, dissolution rate and improvement of oral bioavailability of water insoluble nifedipine (NFD) drug with development of their solid dispersion by using solvent evaporation method. Solid dispersion of nifdipine was prepared by solvent evaporation method using polyethylene glycol 6000 (PEG- 6000), PVP K40000 in different drug: polymer ratios (1:2, 1:3, 1:4, 1:5) and tween-80 as surfactant was used. The solid dispersion of NFD was evaluated, using FTIR, X‐ray diffraction, DSC and in-vitro dissolution method. The X-ray diffraction pattern represented the amorphous form; FTIR indicated no any interaction was found between drug-polymer and DSC respectively. The solid dispersion with PVP K40000 at 1:4 ratio, and was exhibited significant higher drug release profile when compared to pure drug and marketed product. The % cumulative drug release of solid dispersion and marketed product of nifedipine was found 98.46±.20% and 76.23.46±.74%. The solid dispersion of nifedipine was found stable, under stability study in accelerated storage conditions. Solid dispersion of nifedipine containing PVP K40000 polymer, showed significant improvement in the drug release profile as compared to nifedipine pure and marketed product. It could be used for the enhancement solubility, dissolution rate and bioavailability of nifedipine.

Keywords: Nifedipine, Solid Dispersion, PEG 6000, Tween-80, PVP.

A contribution to the valorization ‎of two medicinal plants: Atriplex ‎halimus sub. Sp. Schweinfurthii ‎and Bunium incrassatum, growing ‎in the region of M’sila (north-east ‎Algeria)

Dehimi Khadidja, Djoudi Zouina, Boulaouad Anis, Maadadi Abd Raouf, Dahamna Saliha, Khennouf Seddik

Abstract:
Atriplex halimus and Bunium incrassatum were extracted using solvents from different polarities (water, methanol, acetone and hexane). To evaluate the antioxidant abilities of the extracts, three in vitro test systems were employed: DPPH scavenging assay, β- carotene bleaching test and the reducing power assay. Extractions using acetone were the richest in polyphenols, while hexane fractions from both plants were found to contain the highest amounts of flavonoids. Tannins were more frequent in acetone fraction from AH. The best scavenging activity against DPPH radical was obtained by hexane extract from AH, followed by acetone and methanol extracts from the same plant. BI fractions showed a weak scavenging activity with IC₅₀ values higher than 20 mg.mL^-1. Acetone fractions showed the best iron reducing activity in both plants. In the BCB assay, hexane fraction from AH showed an excellent activity which was very close to that of butylated hydroxytoluene.

Keywords: Atriplex Halimus, Bunium Incrassatum, Polyphenols, DPPH, Reducing Power, β- Carotene Bleaching.

Improved antibacterial activity of ‎honey, propolis and beeswax-‎sodium carboxymethyl cellulose ‎composite hydrogel

Mohamed Hamdi, Baghdad Khiati, Moussa Ahmed

Abstract:

Honey, propolis, and beeswax are natural products that have been used in alternative medicine and traditional practices. This study aimed to develop an antibiotic hydrogel containing propolis, honey, and beeswax and evaluation of its antibacterial potentials. Fourier transform infrared (FTIR) analysis was employed to characterise the NaCMC-H-P-BW hydrogel. Besides, the antibacterial activity of composite hydrogel was determined by using agar well diffusion assay against Staphylococcus aureus and Escherichia coli, and the zone of inhibition was measured in terms of millimeters. A topical cream containing 1% silver sulfadiazine was used as a positive control and distilled water will be used as the negative control. Fourier transform infrared spectroscopy (FTIR) analysis suggested the formation of strong intermolecular interactions as hydrogen, oxygen, and carbon attractions between polymer and propolis, honey and beeswax. The antibacterial properties showed the inhibition activity against Staphylococcus aureus (23.10±4.60 mm) and E. coli (22.95±4.76 mm). Moreover, the inhibition activity observed for the positive control (silver sulfadiazine) was comparatively less compared to NaCMC-H-P-BW hydrogel Staphylococcus aureus (8.25±0.95) and Escherichia coli (9.30±1.53). These studies suggest that the topical formulation could be used as an antibacterial topical apitherapeutic product.

Keywords: NaCMC, Honey, Propolis, Beeswax, Antibacterial Activity.

Formulation and evaluation of ‎teneligliptin-loaded mucoadhesive ‎microspheres

Jameel Ahmed S Mulla, Vijayanand R Aralelimath, Omkar Tipugade, Shreyasi S Shinde, Nisha G Tetgure, Ayesha A Mulla, Dinesh D Gavali

Abstract:
The mucoadhesive microspheres are one of the most promising novel techniques for drug delivery. Mucoadhesive systems provide a sustained drug release method, enhancing drug absorption in a site‐specific manner. This study aims to prepare teneligliptin mucoadhesive microspheres to increase the residence time in the gastric and offers control release. The teneligliptin mucoadhesive microspheres are prepared by ionotropic external gelation technique using sodium alginate, HPMC K4, HPMC K15, HPMC K100, xanthan gum, guar gum, and carbopol 934. All mucoadhesive microspheres after preparation were characterized for percentage yield, particle size, drug entrapment efficiency, mucoadhesive test, and in vitro release. The results obtained are differed depending on the concentration of polymers and ratios of drug to polymers.

Keywords: Diabetes, Teneligliptin, Mucoadhesive, Microspheres, In Vitro Release Study.

Indian Journal of

Novel Drug Delivery ISSN 0975-5500

Indian Journal of Novel Drug Delivery ISSN 0975-5500