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B. Soujanya ¹, J. Geethanjali ², D. Mounika ³, V. Saikishore ⁴

Affiliations
1 Bapatla College of Pharmacy, Bapatla, IN
2 Department of Analysis, Bapatla College of Pharmacy, Bapatla, IN
3 Department of Pharmaceutics, Bapatla College of Pharmacy, Bapatla, IN
4 Department of Pharmaceutics, Bapatla College of Pharmacy, Bapatla-522101, Guntur, Andhra Pradesh, IN

Abstract

In the present work, eudragitL100and Eudragit RLPO films were prepared and evaluated as rate controlling membrane for transdermal drug delivery systems. Dibutyl phthalate or propylene glycol at a concentration of 15w/w of the polymer was used as a plasticizer in the preparation of eudragitL100and Eudragit RLPO films. Casting on mercury surface technique was employed for preparation of eudragitL100and Eudragit RLPO films. The dry films were evaluated for physical appearance, water vapour transmission, drug diffusion and permeability coefficient. Both water vapour transmissions, drug diffusion rate followed zero-order kinetics. The mechanism of drug release was governed by peppas model. The diffusion exponent of release profiles (slope) has a value of 1.056-1.071 (n>1), which indicates super case ц transport diffusion. The results obtained in the present study thus indicate that the polymer and solvents used in the preparation of films have shown significant influence on the water vapour transmission, drug diffusion and permeability of the films.

Keywords

Polymer, Solvents, Water Vapour Transmission, Drug Diffusion and Permeability Coefficient.

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Y. Saikumar ¹, V. Saikishore ², K. Pavani ², D. T. Sairam ², A. Sindhura ²

Affiliations
1 Department of Pharmaceutics, Bapatla College of Pharmacy, Bapatla, Guntur (Dt), Andhra Pradesh-522101, IN
2 Department of Pharmaceutics, Bapatla College of Pharmacy, Bapatla, Guntur (Dt), Andhra Pradesh-522101, IN

Abstract

The transdermal route has been recognized as one of the highly potential routes of systemic drug delivery and provides the advantage of avoidance of the first-pass effect, ease of use and withdrawal (in case of side effects), and better patient compliance. However, the major limitation of this route is the difficulty of permeation of drug through the skin. The skin is very effective as a selective penetration barrier. The stratum corneum provides the greatest resistance to penetration, and it is the rate-limiting step in percutaneous absorption. Penetration enhancers are the substances that facilitate the absorption of penetrant through the skin by temporarily diminishing the impermeability of the skin. Ideally, these materials should be pharmacologically inert, nontoxic, nonirritating, nonallergenic, compatible with the drug and excipients, odorless, tasteless, colorless, and inexpensive and have good solvent properties. No single penetration enhancer can possess all the required properties. However, many enhancers exhibit many of these attributes, and they have been tested in clinics or in research laboratories. Several scientists are engaged in transdermal permeation studies using various enhancers for several drug moieties. The present review includes the classification of permeation enhancers and their mechanism of action; thus, it will help in the selection of a suitable enhancer(s) for improving the transdermal permeation of poorly absorbed drugs.

Keywords

Transdermal Delivery, Skin Penetration, Percutaneous Absorption, Penetration Enhancer.

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P. Sivannarayana ¹, A. Prameela Rani ², V. Saikishore ³, Ch. VenuBabu ⁴, V. SriRekha ⁴

Affiliations
1 VishwaBharathi College of Pharmaceutical Sciences, Perecherla, Guntur, IN
2 College of Pharmaceutical Sciences, ANU, Guntur, IN
3 Baptla College of Pharmacy, Bapatla, Guntur (Dt), IN
4 Vishwa Bharathi College o f Pharmaceutical Sciences, Perecherla, Guntur, IN

Abstract

In vesicular drug carrier systems transfersomes (ultra-deformable carrier systems) are novel carriers, are composed of phospholipid, surfactant, water enhanced transdermal drug delivery systems(TDDS). Transfersomes are efficient in delivering the low molecular weight and as well as high molecular weight drugs through skin, consisting of hydrophobic and hydrophilic moieties together and has a result wide range of solubility. This vesicular transfersomes can deform and pass through narrow constriction (about 10 times less than their own diameter) without measurable loss, This high deformability gives better penetration of intact vesicles, and transfersomes are highly flexibility of particles, so drug targeting can be achieved by this type of delivery systems. Recently various approaches have been used to augment the transdermal delivery of bioactive, they include iontophoresis, electrophoresis, sonophorosis, chemical permeation enhancers, microneedle systems. eg: Analgesics, Anesthetic, Corticosteroids, sex Harmones, Anticancer, Insulin. transferosomes have beneficial advantages over the vesicular systems, higher stability, systemic drug release possible to other than vesicular systems.

Keywords

Transfersomes, Ultra-Deformable Carrier, Anticancer, Higher Stability, Flexibility.

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M. Sukanya ¹, V. Saikishore ², P. Y. Shanmukha ², K. Srikanth ²

Affiliations
1 Bapatla College of Pharmacy, Bapatla-522101, Andhra Pradesh, IN
2 Bapatla College of Pharmacy, Bapatla-522101, Andhra Pradesh, IN

Abstract

Pulsatile drug delivery systems (PDDS) are gaining importance in the field of pharmaceutical technology as these systems deliver the right dose at specific time at a specific site. These systems are designed according to the circadian rhythm of the body. The principle rationale for the use of pulsatile release is for the drugs where a constant drug release, i.e., a zero-order release is not desired. The release of the drug as a pulse after a lag time has to be designed in such a way that a complete and rapid drug release follows the lag time. Advantages of the pulsatile drug delivery system are reduced dose frequency; reduce side effects, drug targeting to specific site like colon and many more. Diseases wherein PDDS are promising include asthma, peptic ulcer, cardiovascular diseases, arthritis, attention deficit syndrome in children, and hypercholesterolemia. In pursuit of pulsatile release, various design strategies have been proposed, mainly including time controlling, stimuli induced, externally regulated and multiparticulate formulations. This review will cover methods with different polymeric systems like time controlling, internal stimuli induced (temperature induced and chemical stimuli-induced), and external induced (magnetic fields, ultrasound, electric fields and light stimulation) and multiparticulate system. The current article focuses on the diseases requiring PDDS, methodologies involved for the existing systems, recent update and PDDS product currently available in the market.

Keywords

Pulsatile Drug Release, Lag Time, Circadian Rhythm, Stimuli Induced, Multiparticulate.

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N. Sandhya Rani ¹, M. Teja Krishna ², V. Saikishore ¹

Affiliations
1 Dept. of Pharmaceutics, Bapatla College of Pharmacy, Bapatla-522101, Andhra Pradesh, IN
2 Opp. KDCC Bank, Ghantasala Post & Mandal Krishna-521133, IN

Abstract

Mucoadhesive microcapsules of Glipizide were prepared for reducing the dosing frequency , to improve the patience compliance and to obtain control release.Glipizide microcapsules with a coat consisting of alginate and sweet potato starches were prepared by employing ionic gelation and emulsification ionotropic gelation techniques. The microcapsules were evaluated for flow properties, Carr's index, hausner factor, microencapsulation efficiency, drug release characteristics, surface characteristics; compatibility studies and mucoadhesive properties .These two methods gave discrete, large sized, free flowing spherical microcapsules without any interactions. Glipizide release from the microcapsules was slow and followed zero order kinetics and followed non-fickian release and depended on the coat: core ratio and the method employed in the preparation of microcapsules. Among the two methods emulsification ionotropic gelation technique was found to be more suitable for slow and complete release of Glipizide over a long period of time. These microcapsules exhibited good mucoadhesive property in the in vitro wash-off test. These Mucoadhesive microcapsules are, thus, suitable for oral controlled release of Glipizide.

Keywords

Glipizide, Microcapsules, Ionic Gelation , Emulsification Ionotropic Gelation.

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V. Saikishore ¹, G. Srikanth ¹, Ch. Pooja ¹, Y. Mrudula ¹, R. Pavani ¹, Ch. Jyosthna ¹, C. Mayuren ¹

Affiliations
1 Dept. of Pharmaceutics, Bapatla College of Pharmacy, Bapatla-522101, Andhra Pradesh, IN

Abstract

Glibenclamide is a second generation antidiabetic drug used for the treatment of Type -II Diabetes. Glibenclamide is practically insoluble in water and so possesses poor solubility, GI absorption and bioavailability. In order to improve the dissolution rate and thereby the absorption, fast dissolving tablets of Glibenclamide were prepared using superdisintegrants by direct compression. To study the influence of concentration of the sodium starch glycolate on the performance of Glibenclamide, a set of four formulations (F1, F2, F3, F4) were prepared using four different concentrations of sodium starch glycolate (2%, 3%, 4%&amp;5%w/w) respectively. The formulation prepared with 5%w/w of sodium starch glycolate was offered relatively rapid release of Glibenclamide when compared with other concentrations employed in this investigation. To study the influence of superdisintegrants on the performance of Glibenclamide, a set of three formulations (F4, F5 and F6) were prepared using three different superdisintegrants viz, Sodium starchglycolate(5%),Ac-Di-Sol(5%), Crospovidone (5%) respectively. Based on the dissolution rate, superdisintegrants can be rated as Sodium starchglycolate < Ac-Di-Sol < Crospovidone. Nature and concentration of the superdisintegrant showed influence on the rate of dissolution. The formulated tablets were subjected to various quality control tests and the results were complied with the pharmacopoeial standards. The drug release profiles followed first-order kinetics. The rate of drug release was found to be increased by increasing the concentration of the superdisintegrant and found to be highest for tablets formulated with 5%w/w of crospovidone. Blood glucose concentrations for developed formulation at times 1 and 2 hr were significantly lower than those for pure drug and marketed formulation. There is a correlation between in vivo and in vitro parameters. These correlations indicate that drug hypoglycemic effects are highly controlled by the drug dissolution. The higher the dissolution the higher is the corresponding in vivo parameter.

Keywords

Glibenclamide, Sodium Starchglycolate, AC-DI-SOL, Crospovidone, Hypoglycemic Effects.

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N. Sandhya Rani ¹, M. Teja Krishna ¹, V. Saikishore ¹

Affiliations
1 Dept. of Pharmaceutics, Bapatla College of Pharmacy, Bapatla-522101, Andhra Pradesh, IN

Abstract

Mucoadhesive microcapsules of Glipizide were prepared for reducing the dosing frequency , to improve the patience compliance and to obtain control release.Glipizide microcapsules with a coat consisting of alginate and sweet potato starches were prepared by employing ionic gelation and emulsification ionotropic gelation techniques. The microcapsules were evaluated for flow properties, Carr's index, hausner factor, microencapsulation efficiency, drug release characteristics, surface characteristics; compatibility studies and mucoadhesive properties .These two methods gave discrete, large sized, free flowing spherical microcapsules without any interactions. Glipizide release from the microcapsules was slow and followed zero order kinetics and followed non-fickian release and depended on the coat: core ratio and the method employed in the preparation of microcapsules. Among the two methods emulsification ionotropic gelation technique was found to be more suitable for slow and complete release of Glipizide over a long period of time.

These microcapsules exhibited good mucoadhesive property in the in-vitro washoff test. These Mucoadhesive microcapsules are, thus, suitable for oral controlled release of Glipizide.

Keywords

Glipizide, Microcapsules, Ionic Gelation , Emulsification Ionotropic Gelation.

Full Text