Approaches to Creating and Past Successful Attempts on Microspheres: A Primer for Aspiring Researchers

 

Kappala Sailaja, Hindustan Abdul Ahad, Haranath Chinthaginjala, Renuka Gudisipalli,

Sugali Indravath Rajyalakshmi, Yamuna Vagganagari

Department of Industrial Pharmacy, Raghavendra Institute of Pharmaceutical Education and Research

(RIPER) - Autonomous, K.R. Palli Cross, Chiyyedu (P), Ananthapuramu - 515721, AP, India.

*Corresponding Author E-mail:

 

ABSTRACT:

The work was aimed at the gathering and projection of literature on microspheres. A targeted drug delivery system is intended to increase the concentration of medication in the areas of interest while reducing its concentration in the rest of the body. Thus, the drug is localized at the target site. It does not affect the surrounding tissues. Carriers have therefore proven to be a useful approach to drug delivery since the drug is coupled with a carrier particle such as microspheres, nanoparticles, liposomes, niosomes, and so on, that controls the release and absorption of the drug. A microsphere is a free-flowing powder consisting of proteins or synthetic polymers that are biodegradable in nature and, ideally, have a particle size of under 200 m. If it is modified, it is a reliable way to deliver the drug to the target site with high specificity and to maintain the desired concentration without unintended side effects. As a result of their long-term release, microspheres have been receiving a lot of attention, especially for their ability to target anticancer drugs to the tumor. By combining microspheres with a variety of other strategies, microspheres will have a key role in the delivery of pharmaceuticals, especially in diseased cell sorting, diagnostics, gene delivery, and safe, targeted, and effective in vivo delivery. This article will help research to get a quick reference to the past work done on microsphere dosage forms.

 

KEYWORDS: Delivery, microspheres, release, review, target.

 

 


INTRODUCTION:

In the novel drug delivery system, a drug is delivered at a rate determined by the needs of the body during the duration of treatment, and its active ingredients are delivered to the site of action. Currently, no drug delivery system can fulfill all the lofty goals, however, sincere efforts are being made to achieve them through novel approaches to drug delivery1.

 

Different routes of administration are available for controlled and targeted drug delivery, resulting in a variety of novel drug delivery systems. In recent years, there has been considerable interest in using microspheres for drug delivery2. In terms of sustained or controlled release, microspheres of biodegradable and nonbiodegradable polymers have been studied. Microspheres are characterized by a microphase separation morphology, which acts as a catalyst to control degradation rate and drug release3.

 

Methods for preparation of microspheres:

The following techniques were adopted in making microspheres4,5:

1. Single emulsion techniques

2. Double emulsification techniques

3. Polymerization

    a. Normal polymerization

·     Bulk

·     Suspension

·     Emulsion

    b. Inter-facial polymerization

4. Coacervation phase septation technique

5. Spray drying and spray congealing technique

6. Solvent evaporation method

7. Solution- strengthening distribution method

8. Wax coating and Hot-melt method

 

Pharmaceutical application of microspheres

The main inputs of microspheres in pharma field are as follows6.

·      Vaccine delivery

·      Monoclonal antibodies

·      Imaging

·      Topical porous microsphere

·      Nasal drug delivery

·      Oral drug delivery

·      Targeting drug delivery

·      Gastro-retentive controlled delivery system

·      Bio-medical applications

·      Pharmaceutical application

 

Advantages of microspheres:

Microspheres have these merits7

·      Microspheres show constant and long-lasting therapeutic action.

·      Dosing frequency can be changed, and so we can improve patient compliance.

·      Due to their spherical shape and smaller size, they could be injected into the body.

·      good bioavailability and low risk of side effects

·      Microsphere morphology all depends on controllable variability in degradation and drug release.

 

Disadvantages of microspheres:

The demerits of microspheres are as follows8

·      The modified release from the formulations

·      The release rate of the controlled release dosage form may vary due to a variety of factors, like food and the rate of transit through the gut.

·      differences in the release rate from one dose to another.

·      Controlled release formulations generally contain a higher drug load and, thus, any loss of integrity of the release characteristics of the dosage form may lead to potential toxicity.

·      Dosage forms of this kind should not be crushed or chewed.

 

For quick reference to the researchers who want to work on microspheres, Table 1 summarizes previous successful attempts on microspheres.


 

Table 1: Past work done on drugs and polymers in making microspheres

Drug

Polymer

Reference

Doxorubicin

Poly lactic acid (PLA)

9Juni et al., 1985

Diclofenac sodium

Albumin

10Hideshi et al., 1990

5-fluro uracil

PLA, and Polyglycolide (PGA)

11Moritera et al., 1991

Methotrexate

Poly anhydride (PA)

12Bhagat etal., 1994

Ofloxacin

Gelatin, poly glycolic acid-co-DL-lactic acid (PGLA)

13Habib et al., 1999

Bupivacaine

PLA, and PLGA

14Kwak et al., 2000

Naltrexone

PLA

15Dinarvand et al., 2003

Metaprolol tartrate

Egg albumin, ethyl cellulose (EC), and Eudragit RL 100

16Rajinikanth et al., 2003

Cyclosporin A

PLA, and PLGA

17B Malaekeh et al., 2005

Ciprofloxacin

Chitosan, and Pectin

18Orhan et al., 2006

Glibenclamide

Mucuna gum

19Amaechi et al., 2007

Diltiazem

Polyethylene glycol 600

20Nappinnai et al., 2007

Meloxicam

Poly lactic acid

21Im et al., 2008

Ketorolac tromethamine

Polycaprolactone (PCL), and PLA

22Sinha et al., 2008

NNMDA-curcumin

PCL

23Sankavarapu et al., 2009

Theophylline, xanthine derivative

PCL

24Jelvehgari et al., 2010

Tinidazole

Bovine serum albumin

25Parashar et al., 2010

Aceclofenac

PLA

26Chandiran et al., 2010

Zopiclone

PCL

27Swapna et al., 2010

Idarubicin

EC, and HPMC

28Ganesh et al., 2010

Famotidine

Carboxy Methyl Cellulose

29Arya et al., 2010

Loxoprofen

EC

30Venkatesan et al., 2011

Theophylline

Chitosan, sodium alginate, and egg albumin

31Jelvehgari et al., 2011

Tetanus toxoid

Chitosan

32Arthanari et al., 2011

Caffeine

Bovine serum albumin

33Malviya et al., 2011

Methotrexate

PLGA

34Sibeko et al., 2012

Ibuprofen

poly(hydroxybutyrate-co-hydroxyvalerate) (PHBV), and PLA

35Bazzo et al., 2012

Ropinirole HCl

PLGA

36Madan et al., 2013

Infliximab

PLGA

37Gokhale et al., 2013

Enalapril maleate

Egg albumin

38Nanjwade et al., 2014

Aspirin

EC

39Reddy et al., 2014

Isoniazid

Hydroxyethyl methacrylate (HEMA)

40Jafari et al., 2015

Lovastatin

PLA

41Guan et al., 2015.

Indomethacin

Egg albumin, EC, and Eudragit L 100

42Bose et al., 2016

Mefenamic acid

Ethyl cellulose

43Anusha et al., 2016

Venlafaxine HCl

Chitosan

44Jain et al., 2016

Ropivacaine

Chitosan

45Ni et al., 2016

Simvastatin

PLGA

46Masaeli et al., 2016

paracetamol

chitosan-graft-polyacrylamide (CS-g-PAM)

47Bulut et al., 2016

Nateglinide

Olibanum gum, Guar gum (GG), and sodium alginate

48Pandey et al., 2016

Insulin

HEMA

49Kenechukwu et al., 2016

Losartan potassium

EC

50Khairnar et al., 2017

Azithromycin

Xanthan gum, and GG

51Bhattacharjee et al., 2018

Ivabradine HCl (IBH)

Egg albumin, and EC

52Singh et al., 2019

Metformin hydrochloride 

Khaya gum, and sodium alginate

53Ozoude et al., 2020

Pentazocin

EC

54Jabar et al., 2021

Ranitidine

Carbopol 934, chitosan and sodium alginate

55Palanivelu et al., 2021

 


CONCLUSION:

Microsphere has the advantage of target specificity and better patient compliance compared to many other types of drug delivery systems. From the foregoing, it is concluded that microspheres are a promising candidate for sustained and targeted drug delivery in various targeted organs. Aside from drug delivery, microspheres are also used for imaging tumors, detecting biomolecule interactions for diagnostics, and cancer treatment, among other things. Therefore, in the future, microspheres will play a very important role in the advancement of medicine. Researchers will be provided with a quick reference to past literature on microspheres through this review.

 

ACKNOWLEDGMENTS:

The authors are thankful to the college management for the encouragement and the support.

 

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Received on 03.02.2022        Modified on 18.02.2022

Accepted on 27.02.2022   ©AandV Publications All Right Reserved

Res.  J. Pharma. Dosage Forms and Tech.2022; 14(3):245-248.

DOI: 10.52711/0975-4377.2022.00040