The aim of the study was the Development and Evaluation of Floating alginate beads of Esomeprazole. The

floating alginate beads of Esomeprazole (F1–F6) were prepared in six different batches using varying

concentration of sodium alginate and HPMC K4M using inotropic gelation technique. The floating alginate

beads of Esomeprazole (F1–F6) were extensively evaluated. Micrometric properties such as angle of repose, bulk

density, tapped density, Carr’s index, and Hausner’s ratio confirmed good flow and packing behavior across all

formulations, with F5 exhibiting the most favorable characteristics. The drug entrapment efficiency increased

with polymer concentration, reaching a maximum of 87.96 ± 1.05% for F5.Floating lag time decreased with

stability and drug dissolution

A floating drug delivery system (FDDS) is a type of drug delivery system designed to prolong the residence time

of drugs within the gastrointestinal (GI) tract, particularly the stomach. The primary objective of FDDS is to

enhance the bioavailability and efficacy of drugs, particularly those with narrow absorption windows or those

that degrade in the acidic environment of the stomach.

In FDDS, the drug is typically incorporated into a formulation that possesses low density or contains gas-

generating agents, allowing it to float on the gastric contents after ingestion. This buoyancy ensures that the drug

bead structure. Calcium salts, such as calcium chloride or calcium carbonate, are commonly used as cross-linking

agents to gel the alginate and form stable beads. Drugs or other active ingredients can be incorporated into the

alginate matrix to achieve controlled release or targeted delivery. Additional excipients such as gel-forming

agents, pore-forming agents, and release modifiers may be included to optimize bead characteristics and drug

release kinetics.

Gastroretentive floating beads are small, solid and free flowing particulate carriers, on which the drug is coated

or encapsulated in the core of beads. Beads can provide controlled / sustained release properties and as such

bioavailability of drugs are enhanced. Gastro retentive beads are not just to sustain the drug release, but also to

enhance gastric residence of the dosage forms until the entire drugs are completely released at the desired period

Esomeprazole was obtained as gift samples from Cipla Ltd, Goa, HPMC purchased from Colorcon Asia Pvt Ltd,

Sodium Alginate purchased from S.D. Fine Chem. Ltd, all other chemicals are analytical grade.

Melting point of Esomeprazole was determined by capillary method. Fine powder of Esomeprazole was filled

in the glass capillary tube which was sealed at end. The capillary tube is tied to thermometer and the thermometer

was placed in melting point apparatus. The powder at what temperature it will melt was noticed as melting

temperature of drug.

Drug-excipient compatibility studies are an essential part of preformulation and formulation development

processes in the pharmaceutical industry. These studies assess the compatibility of a drug substance with various

excipients that are used to formulate the final dosage form. he primary purpose of drug-excipient compatibility

studies is to evaluate potential interactions between the drug substance and excipients. These studies aim to

identify any chemical, physical, or mechanical interactions that could affect the stability, efficacy, or safety of

the final dosage form. By assessing compatibility early in the development process, formulation scientists can

make informed decisions regarding excipient selection, formulation design, and process optimization.

Compatibility study of drug with the excipients was determined by I.R. Spectroscopy (Shimadzu, Japan). The

pellets were prepared at high compaction pressure by using KBr and the ratio of sample to KBr is 1:100. The

a uniform drug solution. To this, the required concentration of Sodium Alginate (as per the formulation F1–F6)

was slowly added with continuous stirring to obtain a homogenous polymeric solution. For formulations F4 to

F6, the required amount of HPMC K4M was also incorporated as a secondary polymer to enhance the gel

strength and sustain the drug release. To impart floating properties, sodium bicarbonate was added to the

polymer-drug dispersion and mixed thoroughly. The final mixture was allowed to hydrate for 30 minutes to

remove entrapped air and ensure complete polymer swelling. The prepared dispersion was then extruded

air-dried at room temperature for 24 hours and stored in airtight containers for further evaluation. The

composition of different formulation of Esomeprazole floating beads is shown in the table

1.

Table 1: Formulation of Floating Beads of Esomeprazole

To determine the drug entrapment efficiency (%DEE) of the prepared floating alginate beads of Esomeprazole,

a known weight of the dried beads (usually 100 mg) was accurately weighed and crushed using a mortar and

pestle to obtain a fine powder. This powder was then transferred into a 100 ml volumetric flask containing 0.1 N

hydrochloric acid (pH 1.2), which serves as the dissolution medium. The mixture was sonicated for 30 minutes to

ensure complete extraction of the entrapped drug and then stirred continuously for another 1 hour using a

magnetic stirrer to achieve thorough drug release from the polymeric matrix. After complete extraction, the

resulting solution was filtered through Whatman filter paper or centrifuged to remove undissolved particles. The

clear filtrate was appropriately diluted and analyzed spectrophotometrically at 301 nm (the λmax of

In this parameter 100 mg of beads formulation were added into the 900 ml dissolution vessel containing 0.1N

HCl at 37

lag time.

In this parameter 100 mg of beads formulation was added into the 900 ml dissolution vessel containing 0.1N

HCl at 37

C. The time for which the formulation remains constantly floating on surface of dissolution medium

was referred as duration of floating.

The particle sizes of drug loaded beads were measured by an optical microscope fitted with an ocular and stage

using following formula.

In-vitro dissolution studies were performed for all the formulations using USP type II apparatus. An accurately

weighed floating alginate beads were taken into 900ml 0.1 N Hcl buffer (pH 1.2). The temperature was

maintained at 37 ± 0.5 C

and stirred at a speed of 50 rpm. At specified time intervals 5 ml of sample was

withdrawn, at the same time 5 ml of fresh dissolution media was added to maintain sink condition. The collected

samples were filtered if necessary and analyzed at 301 nm using UV spectrophotometer against 0.1 N Hcl buffer

(pH 1.2) taken as blank.

The melting point of Esomeprazole was determined by capillary method, melting point of Esomeprazole was

found to be 217 to 220°C. Melting point of drug was compared with pharmacopoeial standards that confirmed

the purity of drug sample.

Table 2: Micromeritics Properties Of Floating Beads (F1 to F6)

Table 3: Characterizations of Floating Beads of Esomeprazole (F1 to F6)

(Values are SD ± Mean of n=3)

release of 91.34% over 12 hours, likely due to increased gel viscosity forming a denser matrix that hindered

complete drug diffusion. These results indicate that the combination of sodium alginate and HPMC K4M

effectively modulates the drug release rate. Among all batches, F5 was found to be the optimized formulation,

providing a balanced and sustained release over 12 hours with the highest cumulative drug release. This

highlights its potential for improved gastric retention and controlled delivery of Esomeprazole. Data for in vitro

drug release of floating beads was shown in figure 2

Figure 2: Comparative In Vitro Dissolution Profile Of Formulation F1 to F6

conditions. The parameters evaluated included floating lag time, total floating time, and percentage drug release.

Floating lag time showed negligible change over the storage period, with values of 33.8 ± 1.4 seconds initially

and 32 ± 0.67 seconds after 3 months. This minimal variation indicates that the formulation retained its buoyancy

properties effectively. The total floating time remained unchanged at more than 12 hours before and after the

storage period, confirming the formulation's ability to maintain prolonged gastric residence over time. The

percentage drug release was 98.26 ± 1.42% at 0 month and slightly decreased to 97.88 ± 1.18% after 3 months.

This minor reduction in drug release is within acceptable limits, suggesting that the drug content and release

profile were not significantly affected by storage.

Overall, the stability study results indicate that formulation F5 is physically and chemically stable over the 3-

month period, maintaining its floating characteristics and drug release profile with no significant degradation or