Gelucire: A Flexible Formulation Excipients

 

Madhulita Panda¹*, M. E. Bhanoji Rao¹, Jnyanaranjan Panda¹, Ch. Niranjan Patra¹, Ganesh Patro²

¹Roland Institute of Pharmceutical Sciences, Berhampur 760010, Ganjam, Odisha.

²College of Pharmaceutical Sciences, Mohuda, Ganjam, Odisha, India.

 

ABSTRACT:

The utility of lipid-based oral formulations has been familiar for many years. There are an enormous variety of polymeric materials used to modify the delivery platform along with enhancement of therapeutic efficacy. Gelucires are a family of lipid-based excipients comprising of glycerides and esters of polyethylene glycol, these two components conferring hydrophobic and hydrophilic properties to the vehicle. Gelucire is used to enhance the drug’s physicochemical properties, as well as controlled release matrices. This review intends to give a critical overview of the published literature on the properties, chemical nature, advantages over other polymers, methods of characterization of gelucire containing formulations, applications and patents containing various grades of gelucires.

 

 

 

INTRODUCTION: 

The significance of lipid-based formulations has increased during the last decades, because they were successfully used in oral drug delivery systems to improve the bioavailability of poorly aqueous soluble drugs, masking of taste using solvent-free processing techniques or improvement of swallowability. Additional reasons for the application of lipids in the formulations may be (1) extension of shelf life by protecting the drug from other ingredients or from the influences of environment, (2) the diminution of gastric irritation, (3) the upgrading of general features like flowability, lubrication performance, compressibility or mechanical resistance. Gelucires are mixtures of glyceride-based materials containing esters of polyethylene glycol which are extensively used in controlled-release matrices for enhancement of the physicochemical properties of the drugs. These polymeric materials contain mixtures of mono-, di- and triglycerides with esters of polyethylene glycol. These components provide hydrophobic as well as hydrophilic natures to the dosage form.

 

The nature and amount of these components can too control the hydrophobicity and discharge properties of drugs in the dosage forms. The rationale of writing the present review on novel lipid carrier Gelucire was to mount up the recent literature with a special emphasis on its properties and applications that have been currently become significant in the field of fast over and above sustained/controlled release drug delivery system. These nonionic, amphiphilic excipients are extensively used in controlled-release matrices for upgrading of the physicochemical properties of the drugs. The review briefly illustrates the properties, applications and recent patents of different grades of Gelucire together with the relevant literature.^1,2

 

Description of Gelucire:

Gelucire is found to be light white waxy solid having light odor except atomized gelucire 70/02 which is available as powders. Gelucires are found to be inert, semi-solid, waxy, amphiphilic excipients with surface-active properties so as to form a fine dispersion or emulsion when exposure to water. Gelucires are characterized by a broad range of melting points, from about 33°C to 70°C and by a HLB values of approximately 1-18. Each Gelucire is characterized by two numbers, the first referring to the nominal melting point of the base and the second is the HLB value. Let us take an example of Gelucire 44/14, the suffixes, 44 and 14, in the excipient trade name refer to its melting point and HLB values respectively. Gelucires with low HLB can be used to decrease the dissolution rate of drugs where as those are with high HLB values mostly used for fast release. Gelucire improves the drug release process by forming hydrogen bonds with the active substance, leading to the formation of stable solids of amorphous drug in microparticles.³

 

Advantages of Gelucire over other polymers used in sustained release formulations⁴:

·      Gelucire has low melt viscosity so that they can prevent the requirement of organic solvents for solubilisation.

·      Absence of toxic impurities for instance residual monomer catalysts and initiators.

·      They are biocompatible as well as biodegradable in nature which is highly crucial.

·      They can prevent gastric irritation by forming a coat around the drugs which are gastric irritant in nature.

·      Acts as carrier for active pharmaceutical ingredients which are sensitive to humidity, light and oxidation.

 

Types of Gelucire:

On the basis of their HLB values, Gelucires are classified into hydrophilic and hydrophobic grades. Gelucire having HLB values lower than 6 are hydrophobic whereas 6-9 are water dispersible and above 9 are hydrophilic. Gelucire 50/13, 44/14, 48/16, 55/18, 35/10 and 48/09 are examples of hydrophilic grades whereas Gelucire 43/01, 39/01, 33/01, 50/02, 54/02 and 64/02 are examples hydrophobic grades. Some examples of Gelucires along with their properties and chemical nature are included in Table 1.

 

 

Figure 1. Different types of gelucires basing upon their HLB values.

Table 1. Overview of the different types of Gelucires ⁵

 

Table 2. A brief reviews on the work done by using Gelucire 43/01

 

The main grades of Gelucire, their key features and applications are illustrated below:

 

1. Gelucire 43/01 (Hard fat EP/NF/JPE)⁶:

Gelucire 43/01 is a hydrophobic lipid with an HLB value of 1 and melting point of °C. It is a combination of saturated triglycerides of diverse fatty acids, viz., C8 - 3%, C10 - 2%, C12 - 29%, C14 - 2%, C16 - 17%, and C18 - 36%. Gelucire 43/01 is used in lipid matrix formulations for sustained release effect. It is used along
with other grades of Gelucire to modify drug release for oral delivery. It is capable of used as a consistency agent in dermal delivery for mineral phase in lipophilic ointment. It acts as a protective carrier for API which is sensitive to oxidation, humidity as well as light. It is used as a lipid binder in melt techniques so that the physicochemical properties and plasticity of the lipid agglomerate offers high resistance to fracture, useful for flash melt and chewable tablets.

 

2. Gelucire 50/13 (Stearoyl macrogol-32 glycerides EP):

Gelucire 50/13 is a non-ionic, water dispersible surfactant consists of PEG-esters, a small quantity glyceride fraction and free PEG. It is obtained by PEGylation of stearoyl glycerides.  It has excellent surf active power to enhance the solubility along with wettability of active pharmaceutical ingredients both in-vitro and in-vivo. It is suitable to use in melt granulation

or agglomeration techniques. It is also appropriate for hard gelatin capsule molding and adsorption onto neutral carrier powders for use in tableting, capsule filling and sachets. It has got extensive application in formulation of solid dispersions as well as self-emulsifying drug delivery systems to enhance solubility, dissolution and bioavailability of drugs.

 

Table 3. A brief-reviews on the work done by using Gelucire 50/13.

 

Table 4. A brief-reviews on the work done by using Gelucire 39/01.

 

3. Gelucire 39/01 [Gattefosse] (semi-synthetic glycerides):

It is a lipophilic carrier chemically consisted of glycerol esters of saturated C12-C18 fatty acids. It is used as a carrier for hard as well as soft gelatin dosage forms. It is bring into play as an excipient, carrier, vehicle and consistency agent.

 

4. Gelucire 44/14 (Lauroyl polyoxyl-32 glycerides):

It is a water dispersible non-ionic surfactant composed of PEG-esters, a minute quantity of glyceride fraction and free PEG. It has an excellent surfactive property which enhances the solubility as well as wettability of active pharmaceutical ingredients. It can also be used as meltable binder. In addition to filling into hard gelatin capsules, it may also be used to make pellets, spheroids, coated fluid air-bed forms, matrix forms or be incorporated into soft gelatin capsules.

 

5. Gelucire 33/01

Gelucire 33/01 is a mixture of glycerides of saturated C8-C18 fatty acids. It is used as a lipid binder in melt techniques for preparation of semisolid matrix, as a consistency increasing agent for topical formulations. It is useful for flash melt and chewable tablets, preparation of pH dependent release formulations.

 

 

 

Table 5. A brief-reviews on the work done by using Gelucire 44/14.

 

Table 6. A brief-reviews on the work done by using Gelucire 33/01.

 

Table 7. A brief-reviews on the work done by using Gelucire 48/16

 

6. Gelucire 48/16:

It is a solid waxy material made up of PEG-32 mono- and diesters of palmitostearic acids and frees PEG-32. It is solid at ambient temperature, making it appropriate for capsule filling and melts processes. It can form a micellar solution when used alone in a simple binary formulation with an active ingredient.

 

Characterization of Gelucire Containing Formulations:

Gelucire containing formulations can be characterized by using several parameters such as physical stability of drug in the matrix systems. Similarly, crystallinity and polymorphic and/or pseudo-polymorphic form of drug in a matrix containing Gelucire can be assessed by differential scanning calorimetry and powder X-ray diffractometry. The nature of interactions between drug and the constituents of the polymeric matrix can be determined by Diffuse reflectance infrared fourier transform spectroscopy. Alternatively, hot stage microscopy, hot stage polarizing microscopy and scanning electron microscopy are the other techniques available for the evaluation of Gelucire containing formulations.⁷³

 

Patents on Gelucire based formulations:

Due to wide applications of different grades of gelucire there are many patents were filed. Patents containing various grades of gelucires such as 43/01, 37/02, 50/02, 54/02, 64/02, 62/05, 35/10, 53/10, 50/13, 44/14, and 48/16 are depicted in Table 7. They are used in different formulation of drugs with miscellaneous applications such as enhancement of absorption, solubility, bioavailability, lipid based nanocarrier for cancer treatment, biphasic formulation, semi solid formulation, solid state solution and dispersions.

 

Table 8. A brief-reviews on the Patents by using different grades of Gelucires.

 

CONCLUSION:

From the formulation point of view, understanding about the polymer behavior and its responsibilities in formulations are crucial for the rational development of different dosage forms. The choice of polymeric components in each formulation, either alone or in combination, is a key parameter. By modifying the chemical composition, varying melting points and HLB values can be used to prepare a variety of gelucires. These gelucires with diverse melting points, hydrophilicity and lipophilicity can be used to form a dispersed phase system. The present review has focused a special interest on gelucires due to their unique properties.

 

ACKNOWLEDGMENTS:

The authors express special thanks to Roland Institute of Pharmaceutical Sciences, Berhampur, Odisha for providing basic facilities to carry out this literature survey.

 

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Accepted on 21.06.2022        © RJPT All right reserved

Research J. Pharm. and Tech 2023; 16(2):955-961.